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Sorafenib (BAY 43-9006) inhibiteur de Raf/VEGFR
Réf. CatalogueS7397
Structure chimique
Poids moléculaire: 464.82
Aller à
Contrôle Qualité
Lot :
Pureté :
99.91%
99.91
| Cibles apparentées | ERK p38 MAPK JNK MEK Ras KRas S6 Kinase MAP4K TAK1 Mixed Lineage Kinase |
|---|---|
| Autre Raf Inhibiteurs | LY3009120 Exarafenib (KIN-2787) GDC-0879 Avutometinib (Ro5126766, CH5126766) PLX-4720 AZ 628 SB590885 TAK-632 GW5074 RAF265 (CHIR-265) |
Culture cellulaire, traitement et concentration de travail
| Lignées cellulaires | Type dessai | Concentration | Temps dincubation | Formulation | Description de lactivité | PMID |
|---|---|---|---|---|---|---|
| MV-4-11 | Growth Inhibition Assay | IC50=0.00000303 μM | SANGER | |||
| MONO-MAC-6 | Growth Inhibition Assay | IC50=0.00418 μM | SANGER | |||
| ALL-PO | Growth Inhibition Assay | IC50=0.03184 μM | SANGER | |||
| NKM-1 | Growth Inhibition Assay | IC50=0.07416 μM | SANGER | |||
| CGTH-W-1 | Growth Inhibition Assay | IC50=0.25022 μM | SANGER | |||
| BB65-RCC | Growth Inhibition Assay | IC50=0.47073 μM | SANGER | |||
| NOS-1 | Growth Inhibition Assay | IC50=0.5636 μM | SANGER | |||
| SH-4 | Growth Inhibition Assay | IC50=0.65613 μM | SANGER | |||
| HOP-62 | Growth Inhibition Assay | IC50=0.85088 μM | SANGER | |||
| HCC2998 | Growth Inhibition Assay | IC50=0.88818 μM | SANGER | |||
| GDM-1 | Growth Inhibition Assay | IC50=0.90698 μM | SANGER | |||
| KM12 | Growth Inhibition Assay | IC50=1.02098 μM | SANGER | |||
| LB2518-MEL | Growth Inhibition Assay | IC50=1.20809 μM | SANGER | |||
| NCI-H1436 | Growth Inhibition Assay | IC50=1.21678 μM | SANGER | |||
| EM-2 | Growth Inhibition Assay | IC50=1.35578 μM | SANGER | |||
| LAMA-84 | Growth Inhibition Assay | IC50=1.37648 μM | SANGER | |||
| KG-1 | Growth Inhibition Assay | IC50=1.47935 μM | SANGER | |||
| A388 | Growth Inhibition Assay | IC50=1.59165 μM | SANGER | |||
| no-10 | Growth Inhibition Assay | IC50=1.61726 μM | SANGER | |||
| SF126 | Growth Inhibition Assay | IC50=1.63812 μM | SANGER | |||
| MEG-01 | Growth Inhibition Assay | IC50=1.8098 μM | SANGER | |||
| A3-KAW | Growth Inhibition Assay | IC50=1.8842 μM | SANGER | |||
| D-247MG | Growth Inhibition Assay | IC50=2.1448 μM | SANGER | |||
| OVCAR-4 | Growth Inhibition Assay | IC50=2.21393 μM | SANGER | |||
| NCI-SNU-1 | Growth Inhibition Assay | IC50=2.3162 μM | SANGER | |||
| NCI-H2171 | Growth Inhibition Assay | IC50=2.39764 μM | SANGER | |||
| SIG-M5 | Growth Inhibition Assay | IC50=2.42242 μM | SANGER | |||
| BE-13 | Growth Inhibition Assay | IC50=2.69609 μM | SANGER | |||
| K052 | Growth Inhibition Assay | IC50=2.74616 μM | SANGER | |||
| L-540 | Growth Inhibition Assay | IC50=2.75789 μM | SANGER | |||
| KMOE-2 | Growth Inhibition Assay | IC50=2.8135 μM | SANGER | |||
| MFH-ino | Growth Inhibition Assay | IC50=2.92185 μM | SANGER | |||
| HL-60 | Growth Inhibition Assay | IC50=3.06299 μM | SANGER | |||
| HCC2218 | Growth Inhibition Assay | IC50=3.12003 μM | SANGER | |||
| TE-5 | Growth Inhibition Assay | IC50=3.13162 μM | SANGER | |||
| MZ1-PC | Growth Inhibition Assay | IC50=3.47509 μM | SANGER | |||
| MRK-nu-1 | Growth Inhibition Assay | IC50=3.61468 μM | SANGER | |||
| MZ7-mel | Growth Inhibition Assay | IC50=3.66099 μM | SANGER | |||
| BC-1 | Growth Inhibition Assay | IC50=3.7402 μM | SANGER | |||
| ST486 | Growth Inhibition Assay | IC50=3.83673 μM | SANGER | |||
| KS-1 | Growth Inhibition Assay | IC50=3.88198 μM | SANGER | |||
| SK-NEP-1 | Growth Inhibition Assay | IC50=4.16815 μM | SANGER | |||
| BC-3 | Growth Inhibition Assay | IC50=4.23391 μM | SANGER | |||
| NCI-H1581 | Growth Inhibition Assay | IC50=4.28798 μM | SANGER | |||
| MHH-PREB-1 | Growth Inhibition Assay | IC50=4.40484 μM | SANGER | |||
| NOMO-1 | Growth Inhibition Assay | IC50=4.48905 μM | SANGER | |||
| QIMR-WIL | Growth Inhibition Assay | IC50=5.07294 μM | SANGER | |||
| SF539 | Growth Inhibition Assay | IC50=5.13227 μM | SANGER | |||
| TE-12 | Growth Inhibition Assay | IC50=5.24929 μM | SANGER | |||
| NCI-H510A | Growth Inhibition Assay | IC50=5.41685 μM | SANGER | |||
| JAR | Growth Inhibition Assay | IC50=5.50824 μM | SANGER | |||
| no-11 | Growth Inhibition Assay | IC50=5.73568 μM | SANGER | |||
| BV-173 | Growth Inhibition Assay | IC50=5.95682 μM | SANGER | |||
| SR | Growth Inhibition Assay | IC50=6.00678 μM | SANGER | |||
| MOLT-16 | Growth Inhibition Assay | IC50=6.25266 μM | SANGER | |||
| MZ2-MEL | Growth Inhibition Assay | IC50=6.31839 μM | SANGER | |||
| SW954 | Growth Inhibition Assay | IC50=6.45866 μM | SANGER | |||
| ML-2 | Growth Inhibition Assay | IC50=6.52849 μM | SANGER | |||
| OCI-AML2 | Growth Inhibition Assay | IC50=6.61062 μM | SANGER | |||
| SIMA | Growth Inhibition Assay | IC50=7.00101 μM | SANGER | |||
| DOHH-2 | Growth Inhibition Assay | IC50=7.05676 μM | SANGER | |||
| 697 | Growth Inhibition Assay | IC50=7.05989 μM | SANGER | |||
| NB1 | Growth Inhibition Assay | IC50=7.40407 μM | SANGER | |||
| D-392MG | Growth Inhibition Assay | IC50=7.62663 μM | SANGER | |||
| ES8 | Growth Inhibition Assay | IC50=7.76503 μM | SANGER | |||
| RPMI-8226 | Growth Inhibition Assay | IC50=7.84511 μM | SANGER | |||
| IST-MEL1 | Growth Inhibition Assay | IC50=8.40002 μM | SANGER | |||
| NB14 | Growth Inhibition Assay | IC50=8.63133 μM | SANGER | |||
| HD-MY-Z | Growth Inhibition Assay | IC50=8.63746 μM | SANGER | |||
| TE-10 | Growth Inhibition Assay | IC50=8.76353 μM | SANGER | |||
| LC-1F | Growth Inhibition Assay | IC50=9.10834 μM | SANGER | |||
| OS-RC-2 | Growth Inhibition Assay | IC50=9.11243 μM | SANGER | |||
| NCI-SNU-16 | Growth Inhibition Assay | IC50=9.21026 μM | SANGER | |||
| SHP-77 | Growth Inhibition Assay | IC50=9.71662 μM | SANGER | |||
| A4-Fuk | Growth Inhibition Assay | IC50=9.7561 μM | SANGER | |||
| NB6 | Growth Inhibition Assay | IC50=9.76029 μM | SANGER | |||
| JiyoyeP-2003 | Growth Inhibition Assay | IC50=10.4745 μM | SANGER | |||
| DMS-114 | Growth Inhibition Assay | IC50=10.5441 μM | SANGER | |||
| NB7 | Growth Inhibition Assay | IC50=10.7526 μM | SANGER | |||
| NCI-H747 | Growth Inhibition Assay | IC50=11.1216 μM | SANGER | |||
| HH | Growth Inhibition Assay | IC50=11.3876 μM | SANGER | |||
| EW-18 | Growth Inhibition Assay | IC50=11.9044 μM | SANGER | |||
| CHP-126 | Growth Inhibition Assay | IC50=11.9738 μM | SANGER | |||
| NTERA-S-cl-D1 | Growth Inhibition Assay | IC50=12.0278 μM | SANGER | |||
| DEL | Growth Inhibition Assay | IC50=12.0985 μM | SANGER | |||
| LU-139 | Growth Inhibition Assay | IC50=12.5413 μM | SANGER | |||
| P30-OHK | Growth Inhibition Assay | IC50=12.5479 μM | SANGER | |||
| NCI-H1522 | Growth Inhibition Assay | IC50=12.746 μM | SANGER | |||
| NCI-H1299 | Growth Inhibition Assay | IC50=13.2911 μM | SANGER | |||
| UACC-257 | Growth Inhibition Assay | IC50=13.5126 μM | SANGER | |||
| Calu-6 | Growth Inhibition Assay | IC50=13.6046 μM | SANGER | |||
| NCI-H1882 | Growth Inhibition Assay | IC50=13.8555 μM | SANGER | |||
| BB30-HNC | Growth Inhibition Assay | IC50=14.0609 μM | SANGER | |||
| ES1 | Growth Inhibition Assay | IC50=14.1551 μM | SANGER | |||
| NCI-H1694 | Growth Inhibition Assay | IC50=14.4811 μM | SANGER | |||
| IST-SL1 | Growth Inhibition Assay | IC50=14.9616 μM | SANGER | |||
| ECC4 | Growth Inhibition Assay | IC50=15.0558 μM | SANGER | |||
| MDA-MB-134-VI | Growth Inhibition Assay | IC50=15.4131 μM | SANGER | |||
| SCH | Growth Inhibition Assay | IC50=15.4728 μM | SANGER | |||
| SK-N-FI | Growth Inhibition Assay | IC50=15.6534 μM | SANGER | |||
| HDLM-2 | Growth Inhibition Assay | IC50=16.0714 μM | SANGER | |||
| Ramos-2G6-4C10 | Growth Inhibition Assay | IC50=16.1297 μM | SANGER | |||
| EW-24 | Growth Inhibition Assay | IC50=16.1661 μM | SANGER | |||
| NCI-H2141 | Growth Inhibition Assay | IC50=16.189 μM | SANGER | |||
| LC4-1 | Growth Inhibition Assay | IC50=16.6119 μM | SANGER | |||
| HT-144 | Growth Inhibition Assay | IC50=17.006 μM | SANGER | |||
| SK-MEL-1 | Growth Inhibition Assay | IC50=17.0072 μM | SANGER | |||
| SCC-15 | Growth Inhibition Assay | IC50=17.1638 μM | SANGER | |||
| C8166 | Growth Inhibition Assay | IC50=17.6833 μM | SANGER | |||
| GOTO | Growth Inhibition Assay | IC50=17.8344 μM | SANGER | |||
| COR-L279 | Growth Inhibition Assay | IC50=18.1362 μM | SANGER | |||
| K-562 | Growth Inhibition Assay | IC50=18.7143 μM | SANGER | |||
| ES3 | Growth Inhibition Assay | IC50=18.8041 μM | SANGER | |||
| LU-165 | Growth Inhibition Assay | IC50=19.7008 μM | SANGER | |||
| KM-H2 | Growth Inhibition Assay | IC50=20.3184 μM | SANGER | |||
| RL | Growth Inhibition Assay | IC50=20.9692 μM | SANGER | |||
| EW-3 | Growth Inhibition Assay | IC50=21.1889 μM | SANGER | |||
| A101D | Growth Inhibition Assay | IC50=21.3752 μM | SANGER | |||
| HUTU-80 | Growth Inhibition Assay | IC50=21.3946 μM | SANGER | |||
| NCI-H23 | Growth Inhibition Assay | IC50=21.3992 μM | SANGER | |||
| PF-382 | Growth Inhibition Assay | IC50=21.4403 μM | SANGER | |||
| LB373-MEL-D | Growth Inhibition Assay | IC50=21.5615 μM | SANGER | |||
| TE-8 | Growth Inhibition Assay | IC50=21.6394 μM | SANGER | |||
| TE-9 | Growth Inhibition Assay | IC50=21.8513 μM | SANGER | |||
| Daudi | Growth Inhibition Assay | IC50=21.9304 μM | SANGER | |||
| D-542MG | Growth Inhibition Assay | IC50=22.0256 μM | SANGER | |||
| U-698-M | Growth Inhibition Assay | IC50=22.4603 μM | SANGER | |||
| ES6 | Growth Inhibition Assay | IC50=22.7366 μM | SANGER | |||
| DU-4475 | Growth Inhibition Assay | IC50=23.8897 μM | SANGER | |||
| ECC12 | Growth Inhibition Assay | IC50=24.2803 μM | SANGER | |||
| C2BBe1 | Growth Inhibition Assay | IC50=24.3239 μM | SANGER | |||
| IST-SL2 | Growth Inhibition Assay | IC50=24.4362 μM | SANGER | |||
| DJM-1 | Growth Inhibition Assay | IC50=24.5221 μM | SANGER | |||
| DMS-153 | Growth Inhibition Assay | IC50=24.8614 μM | SANGER | |||
| NB13 | Growth Inhibition Assay | IC50=25.0265 μM | SANGER | |||
| SK-N-DZ | Growth Inhibition Assay | IC50=26.3414 μM | SANGER | |||
| COR-L88 | Growth Inhibition Assay | IC50=26.5796 μM | SANGER | |||
| LU-65 | Growth Inhibition Assay | IC50=26.8535 μM | SANGER | |||
| TGBC1TKB | Growth Inhibition Assay | IC50=26.9828 μM | SANGER | |||
| THP-1 | Growth Inhibition Assay | IC50=27.2141 μM | SANGER | |||
| ONS-76 | Growth Inhibition Assay | IC50=27.332 μM | SANGER | |||
| LC-2-ad | Growth Inhibition Assay | IC50=27.6231 μM | SANGER | |||
| EW-13 | Growth Inhibition Assay | IC50=29.1746 μM | SANGER | |||
| MS-1 | Growth Inhibition Assay | IC50=30.7278 μM | SANGER | |||
| NCI-H2227 | Growth Inhibition Assay | IC50=30.9806 μM | SANGER | |||
| LXF-289 | Growth Inhibition Assay | IC50=31.4492 μM | SANGER | |||
| MC116 | Growth Inhibition Assay | IC50=32.0826 μM | SANGER | |||
| EVSA-T | Growth Inhibition Assay | IC50=32.2585 μM | SANGER | |||
| CTB-1 | Growth Inhibition Assay | IC50=33.1101 μM | SANGER | |||
| COLO-320-HSR | Growth Inhibition Assay | IC50=33.1603 μM | SANGER | |||
| NCI-H2196 | Growth Inhibition Assay | IC50=33.2557 μM | SANGER | |||
| LB2241-RCC | Growth Inhibition Assay | IC50=33.3135 μM | SANGER | |||
| LS-513 | Growth Inhibition Assay | IC50=33.8638 μM | SANGER | |||
| LP-1 | Growth Inhibition Assay | IC50=33.9956 μM | SANGER | |||
| A253 | Growth Inhibition Assay | IC50=34.2296 μM | SANGER | |||
| SK-MM-2 | Growth Inhibition Assay | IC50=34.9451 μM | SANGER | |||
| NCI-H1963 | Growth Inhibition Assay | IC50=35.3072 μM | SANGER | |||
| MMAC-SF | Growth Inhibition Assay | IC50=35.8785 μM | SANGER | |||
| LB831-BLC | Growth Inhibition Assay | IC50=36.0654 μM | SANGER | |||
| WSU-NHL | Growth Inhibition Assay | IC50=36.164 μM | SANGER | |||
| CESS | Growth Inhibition Assay | IC50=36.2848 μM | SANGER | |||
| NEC8 | Growth Inhibition Assay | IC50=36.5835 μM | SANGER | |||
| KNS-42 | Growth Inhibition Assay | IC50=37.1237 μM | SANGER | |||
| MHH-CALL-2 | Growth Inhibition Assay | IC50=37.1821 μM | SANGER | |||
| K5 | Growth Inhibition Assay | IC50=38.43 μM | SANGER | |||
| CP66-MEL | Growth Inhibition Assay | IC50=39.0733 μM | SANGER | |||
| OPM-2 | Growth Inhibition Assay | IC50=39.8432 μM | SANGER | |||
| IST-MES1 | Growth Inhibition Assay | IC50=40.3096 μM | SANGER | |||
| EC-GI-10 | Growth Inhibition Assay | IC50=41.5805 μM | SANGER | |||
| CTV-1 | Growth Inhibition Assay | IC50=42.8406 μM | SANGER | |||
| DG-75 | Growth Inhibition Assay | IC50=43.7595 μM | SANGER | |||
| KNS-81-FD | Growth Inhibition Assay | IC50=45.4058 μM | SANGER | |||
| NCI-H82 | Growth Inhibition Assay | IC50=45.5758 μM | SANGER | |||
| RPMI-8866 | Growth Inhibition Assay | IC50=46.1873 μM | SANGER | |||
| ACN | Growth Inhibition Assay | IC50=46.434 μM | SANGER | |||
| NCI-H1395 | Growth Inhibition Assay | IC50=46.4756 μM | SANGER | |||
| NCI-H209 | Growth Inhibition Assay | IC50=47.1405 μM | SANGER | |||
| TGW | Growth Inhibition Assay | IC50=49.0791 μM | SANGER | |||
| NCI-H748 | Growth Inhibition Assay | IC50=49.4753 μM | SANGER | |||
| EKVX | Growth Inhibition Assay | IC50=49.6628 μM | SANGER | |||
| MV4-11 | Antiproliferative activity assay | IC50 = 0.00087 μM | 19754199 | |||
| MV4-11 | Cytotoxicity assay | IC50 = 0.00087 μM | 19654408 | |||
| TT | Antiproliferative activity assay | IC50 = 0.0014 μM | 18849971 | |||
| RS4-11 | Function assay | IC50 = 0.002 μM | 19654408 | |||
| MOLM13 | Function assay | IC50 = 0.002 μM | 24641103 | |||
| Sf9 | Function assay | IC50 = 0.003 μM | 21708468 | |||
| RS4-11 | Function assay | IC50 = 0.0032 μM | 19654408 | |||
| MV4-11 | Growth inhibition assay | IC50 = 0.004 μM | 29357250 | |||
| A375 | Function assay | IC50 = 0.0044 μM | 29461827 | |||
| MOLM13 | Antiproliferative activity assay | IC50 = 0.005 μM | 24641103 | |||
| MV4-11 | Function assay | IC50 = 0.007 μM | 23362959 | |||
| MV4-11 | Cytotoxicity assay | IC50 = 0.007 μM | 26342867 | |||
| HEK293 | Function assay | Kd = 0.013 μM | 19754199 | |||
| Kasumi-1 | Antiproliferative activity assay | IC50 = 0.015 μM | 20570526 | |||
| MV4-11 | Antiproliferative activity assay | IC50 = 0.015 μM | 20570526 | |||
| sf9 | Function assay | IC50 = 0.015 μM | 29266937 | |||
| sf9 | Function assay | IC50 = 0.018 μM | 21708468 | |||
| sf9 | Function assay | IC50 = 0.02 μM | 23618709 | |||
| MV4-11 | Antiproliferative activity assay | GI50 = 0.03 μM | 21708468 | |||
| Sf9 | Function assay | IC50 = 0.042 μM | 26081023 | |||
| SF9 | Function assay | IC50 = 0.043 μM | 18473434 | |||
| MV4-11 | Cytotoxicity assay | GI50 = 0.043 μM | 23618709 | |||
| MV4-11 | Function assay | GI50 = 0.043 μM | 26081023 | |||
| SF9 | Function assay | IC50 = 0.044 μM | 26081023 | |||
| SF9 | Function assay | IC50 = 0.054 μM | 21708468 | |||
| SF9 | Function assay | IC50 = 0.054 μM | 23618709 | |||
| MOLM13 | Antiproliferative activity assay | GI50 = 0.056 μM | 21708468 | |||
| MOLM13 | Antiproliferative activity assay | GI50 = 0.056 μM | 22726931 | |||
| MOLM13 | Cytotoxicity assay | GI50 = 0.056 μM | 23618709 | |||
| MOLM-13 | Function assay | GI50 = 0.056 μM | 26081023 | |||
| SF9 | Function assay | IC50 = 0.058 μM | 29266937 | |||
| WM266.4 | Antiproliferative activity assay | IC50 = 0.06 μM | 25496804 | |||
| MDA-MB-231 | Function assay | IC50 = 0.063 μM | 28431342 | |||
| SF9 | Function assay | IC50 = 0.09 μM | 29266937 | |||
| Spodoptera frugiperda | Function assay | IC50 = 0.09 μM | 26922228 | |||
| SF9 | Function assay | IC50 = 0.09 μM | 23562241 | |||
| SF9 | Function assay | IC50 = 0.1 μM | 23442188 | |||
| SF9 | Function assay | IC50 = 0.1 μM | 23442188 | |||
| HEK293 | Function assay | IC50 = 0.12 μM | 26318998 | |||
| MCF7 | Antiproliferative activity assay | IC50 = 0.19 μM | 25496804 | |||
| MV4-11 | Antiproliferative activity human | IC50 = 0.3 μM | 28242553 | |||
| HepG2 | Antiproliferative activity assay | EC50 = 0.302 μM | 27010810 | |||
| THP1 | Antiproliferative activity assay | IC50 = 0.31 μM | 20570526 | |||
| SMMC7721 | Cytotoxicity assay | IC50 = 0.37 μM | 25982075 | |||
| HT-29 | Antiproliferative activity assay | IC50 = 0.39 μM | 25778995 | |||
| sf9 | Function assay | Kd = 0.6 μM | 28109791 | |||
| T47D | Antiproliferative activity assay | IC50 = 0.61 μM | 25778995 | |||
| A549 | Cytotoxicity assay | IC50 = 0.63 μM | 25982075 | |||
| HeLa | Cytotoxicity assay | IC50 = 0.64 μM | 30015070 | |||
| WM3629 | Antiproliferative activity assay | GI50 = 0.65 μM | 20466542 | |||
| SMMC7721 | Antiproliferative activity assay | IC50 = 0.65 μM | 26342134 | |||
| WM3629 | Growth inhibition assay | GI50 = 0.78 μM | 20149658 | |||
| WM3629 | Antiproliferative activity assay | GI50 = 0.78 μM | 26810260 | |||
| MCF7 | Antiproliferative activity assay | IC50 = 0.78 μM | 25778995 | |||
| K562 | Antiproliferative activity assay | IC50 = 0.86 μM | 24315192 | |||
| COLO205 | Antiproliferative activity assay | IC50 = 0.87 μM | 25778995 | |||
| T29 | Cytotoxicity assay | IC50 = 0.9 μM | 26318998 | |||
| MDA-MB-231 | Cytotoxicity assay | IC50 = 0.94 μM | 25086238 | |||
| MDA-MB-231 | Cytotoxicity assay | IC50 = 0.94 μM | 25440879 | |||
| HepG2 | Antiproliferative activity assay | IC50 = 1.06 μM | 29628325 | |||
| BL21(DE3) | Function assay | IC50 = 1.1 μM | 19928858 | |||
| K562 | Antiproliferative activity assay | IC50 = 1.22 μM | 25778995 | |||
| MDA-MB-231 | Growth inhibition assay | GI50 = 1.26 μM | 28088086 | |||
| MDA-MB-231 | Cytotoxicity assay | GI50 = 1.26 μM | 26590508 | |||
| MDA-MB-231 | Antiproliferative activity assay | GI50 = 1.26 μM | 27017549 | |||
| SK-MEL-28 | Antiproliferative activity assay | EC50 = 1.3 μM | 18942827 | |||
| sf9 | Function assay | Kd = 1.3 μM | 28109791 | |||
| F-6-8 | Cytotoxicity assay | IC50 = 1.3 μM | 26318998 | |||
| A549 | Antiproliferative activity assay | IC50 = 1.45 μM | 26342134 | |||
| rhabdomyosarcoma | Antiviral activity assay | EC50 = 1.5 μM | 27288186 | |||
| HL-60(TB) | Growth inhibition assay | GI50 = 1.58 μM | 28088086 | |||
| RPMI8226 | Growth inhibition assay | GI50 = 1.58 μM | 28088086 | |||
| KM12 | Growth inhibition assay | GI50 = 1.58 μM | 28088086 | |||
| LOXIMVI | Growth inhibition assay | GI50 = 1.58 μM | 28088086 | |||
| HCT116 | Growth inhibition assay | GI50 = 1.58 μM | 28088086 | |||
| HOP92 | Growth inhibition assay | GI50 = 1.58 μM | 28088086 | |||
| SF539 | Growth inhibition assay | GI50 = 1.58 μM | 28088086 | |||
| UACC62 | Growth inhibition assay | GI50 = 1.58 μM | 28088086 | |||
| SF295 | Growth inhibition assay | GI50 = 1.58 μM | 28088086 | |||
| MDA-MB-435 | Growth inhibition assay | GI50 = 1.58 μM | 28088086 | |||
| SK-MEL-5 | Growth inhibition assay | GI50 = 1.58 μM | 28088086 | |||
| T47D | Growth inhibition assay | GI50 = 1.58 μM | 28088086 | |||
| RPMI8266 | Cytotoxicity assay | GI50 = 1.58 μM | 26590508 | |||
| HL-60(TB) | Cytotoxicity assay | GI50 = 1.58 μM | 26590508 | |||
| KM12 | Cytotoxicity assay | GI50 = 1.58 μM | 26590508 | |||
| HCT116 | Cytotoxicity assay | GI50 = 1.58 μM | 26590508 | |||
| SF295 | Cytotoxicity assay | GI50 = 1.58 μM | 26590508 | |||
| SF539 | Cytotoxicity assay | GI50 = 1.58 μM | 26590508 | |||
| SK-MEL-2 | Cytotoxicity assay | GI50 = 1.58 μM | 26590508 | |||
| MDA-MB-435 | Cytotoxicity assay | GI50 = 1.58 μM | 26590508 | |||
| SK-MEL-5 | Cytotoxicity assay | GI50 = 1.58 μM | 26590508 | |||
| LOXIMVI | Cytotoxicity assay | GI50 = 1.58 μM | 26590508 | |||
| T47D | Cytotoxicity assay | GI50 = 1.58 μM | 26590508 | |||
| SMMC7721 | Antiproliferative activity assay | IC50 = 1.58 μM | 26753815 | |||
| LOXIMVI | Antiproliferative activity assay | GI50 = 1.58 μM | 27017549 | |||
| UACC62 | Antiproliferative activity assay | GI50 = 1.58 μM | 27017549 | |||
| SK-MEL-5 | Antiproliferative activity assay | GI50 = 1.58 μM | 27017549 | |||
| KM12 | Antiproliferative activity assay | GI50 = 1.58 μM | 27017549 | |||
| MDA-MB-435 | Antiproliferative activity assay | GI50 = 1.58 μM | 27017549 | |||
| SF539 | Antiproliferative activity assay | GI50 = 1.58 μM | 27017549 | |||
| SF295 | Antiproliferative activity assay | GI50 = 1.58 μM | 27017549 | |||
| HCT116 | Antiproliferative activity assay | GI50 = 1.58 μM | 27017549 | |||
| HOP92 | Antiproliferative activity assay | GI50 = 1.58 μM | 27017549 | |||
| RPMI8226 | Antiproliferative activity assay | GI50 = 1.58 μM | 27017549 | |||
| HL-60(TB) | Antiproliferative activity assay | GI50 = 1.58 μM | 27017549 | |||
| T47D | Antiproliferative activity assay | GI50 = 1.58 μM | 27017549 | |||
| 7dF3 | Function assay | IC50 = 1.62 μM | 29266937 | |||
| MDA-MB-435 | Antiproliferative activity assay | IC50 = 1.67 μM | 25778995 | |||
| HL60 | Cytotoxicity assay | IC50 = 1.68 μM | 24858546 | |||
| SW579 | Antiproliferative activity human | IC50 = 1.73 μM | 28242553 | |||
| MCF7 | Antiproliferative activity assay | IC50 = 1.88 μM | 25637123 | |||
| A375P | Antiproliferative activity assay | IC50 = 1.9 μM | 24128410 | |||
| A549 | Cytotoxicity assay | IC50 = 1.92 μM | 24826815 | |||
| HCT116 | Antiproliferative activity assay | IC50 = 2 μM | 22808911 | |||
| MDA-MB-231 | Cytotoxicity assay | IC50 = 2 μM | 23454017 | |||
| NCI-H23 | Growth inhibition assay | GI50 = 2 μM | 28088086 | |||
| NCI-H522 | Growth inhibition assay | GI50 = 2 μM | 28088086 | |||
| HOP62 | Growth inhibition assay | GI50 = 2 μM | 28088086 | |||
| NCI-H226 | Growth inhibition assay | GI50 = 2 μM | 28088086 | |||
| HT-29 | Growth inhibition assay | GI50 = 2 μM | 28088086 | |||
| U251 | Growth inhibition assay | GI50 = 2 μM | 28088086 | |||
| COLO205 | Growth inhibition assay | GI50 = 2 μM | 28088086 | |||
| CCRF-CEM | Growth inhibition assay | GI50 = 2 μM | 28088086 | |||
| MALME-3M | Growth inhibition assay | GI50 = 2 μM | 28088086 | |||
| M14 | Growth inhibition assay | GI50 = 2 μM | 28088086 | |||
| UACC257 | Growth inhibition assay | GI50 = 2 μM | 28088086 | |||
| PC3 | Growth inhibition assay | GI50 = 2 μM | 28088086 | |||
| SK-MEL-2 | Growth inhibition assay | GI50 = 2 μM | 28088086 | |||
| MDA-MB-468 | Growth inhibition assay | GI50 = 2 μM | 28088086 | |||
| CCRF-CEM | Cytotoxicity assay | GI50 = 2 μM | 26590508 | |||
| NCI-H23 | Cytotoxicity assay | GI50 = 2 μM | 26590508 | |||
| NCI-H522 | Cytotoxicity assay | GI50 = 2 μM | 26590508 | |||
| COLO205 | Cytotoxicity assay | GI50 = 2 μM | 26590508 | |||
| HT-29 | Cytotoxicity assay | GI50 = 2 μM | 26590508 | |||
| SK-MEL-28 | Cytotoxicity assay | GI50 = 2 μM | 26590508 | |||
| HOP62 | Cytotoxicity assay | GI50 = 2 μM | 26590508 | |||
| UACC257 | Cytotoxicity assay | GI50 = 2 μM | 26590508 | |||
| NCI-H226 | Cytotoxicity assay | GI50 = 2 μM | 26590508 | |||
| U251 | Cytotoxicity assay | GI50 = 2 μM | 26590508 | |||
| PC3 | Cytotoxicity assay | GI50 = 2 μM | 26590508 | |||
| M14 | Cytotoxicity assay | GI50 = 2 μM | 26590508 | |||
| MDA-MB-468 | Cytotoxicity assay | GI50 = 2 μM | 26590508 | |||
| PC3 | Antiproliferative activity assay | GI50 = 2 μM | 27017549 | |||
| MALME-3M | Antiproliferative activity assay | GI50 = 2 μM | 27017549 | |||
| U251 | Antiproliferative activity assay | GI50 = 2 μM | 27017549 | |||
| UACC257 | Antiproliferative activity assay | GI50 = 2 μM | 27017549 | |||
| SK-MEL-2 | Antiproliferative activity assay | GI50 = 2 μM | 27017549 | |||
| COLO205 | Antiproliferative activity assay | GI50 = 2 μM | 27017549 | |||
| NCI-H23 | Antiproliferative activity assay | GI50 = 2 μM | 27017549 | |||
| HT-29 | Antiproliferative activity assay | GI50 = 2 μM | 27017549 | |||
| M14 | Antiproliferative activity assay | GI50 = 2 μM | 27017549 | |||
| NCI-H226 | Antiproliferative activity assay | GI50 = 2 μM | 27017549 | |||
| HOP62 | Antiproliferative activity assay | GI50 = 2 μM | 27017549 | |||
| MDA-MB-468 | Antiproliferative activity assay | GI50 = 2 μM | 27017549 | |||
| CCRF-CEM | Antiproliferative activity assay | GI50 = 2 μM | 27017549 | |||
| NCI-H522 | Antiproliferative activity assay | GI50 = 2 μM | 27017549 | |||
| A549 | Antiproliferative activity assay | IC50 = 2.02 μM | 26753815 | |||
| MDA-MB-435 | Growth inhibition assay | IC50 = 2.11 μM | 29189002 | |||
| NCI-H460 | Antiproliferative activity assay | IC50 = 2.19 μM | 30216849 | |||
| H460 | Cytotoxicity assay | IC50 = 2.19 μM | 24826815 | |||
| H460 | Cytotoxicity assay | IC50 = 2.19 μM | 25086238 | |||
| H460 | Cytotoxicity assay | IC50 = 2.19 μM | 25440879 | |||
| A375 | Toxicity assay | IC50 = 2.2 μM | 19654408 | |||
| H460 | Antiproliferative activity assay | IC50 = 2.25 μM | 26991938 | |||
| HCT116 | Antiproliferative activity assay | IC50 = 2.3 μM | 23260578 | |||
| MKN45 | Antiproliferative activity assay | IC50 = 2.32 μM | 30216849 | |||
| MKN45 | Cytotoxicity assay | IC50 = 2.32 μM | 24826815 | |||
| MKN45 | Cytotoxicity assay | IC50 = 2.32 μM | 25086238 | |||
| MKN45 | Cytotoxicity assay | IC50 = 2.32 μM | 25440879 | |||
| U937 | Antiproliferative activity assay | GI50 = 2.34 μM | 29459144 | |||
| A375 | Antiproliferative activity assay | IC50 = 2.4 μM | 22808911 | |||
| HeLa | Growth inhibition assay | IC50 = 2.44 μM | 29102175 | |||
| MDA-MB-231 | Cytotoxicity assay | IC50 = 2.5 μM | 22414612 | |||
| MCF7 | Antiproliferative activity assay | IC50 = 2.51 μM | 30216849 | |||
| UO31 | Antiproliferative activity assay | IC50 = 2.51 μM | 30216849 | |||
| NCI-H322M | Growth inhibition assay | GI50 = 2.51 μM | 28088086 | |||
| NCI-H460 | Growth inhibition assay | GI50 = 2.51 μM | 28088086 | |||
| KM12 | Growth inhibition assay | TGI = 2.51 μM | 28088086 | |||
| LOXIMVI | Growth inhibition assay | TGI = 2.51 μM | 28088086 | |||
| EKVX | Growth inhibition assay | GI50 = 2.51 μM | 28088086 | |||
| HCT116 | Growth inhibition assay | TGI = 2.51 μM | 28088086 | |||
| SW620 | Growth inhibition assay | GI50 = 2.51 μM | 28088086 | |||
| SF268 | Growth inhibition assay | GI50 = 2.51 μM | 28088086 | |||
| SF539 | Growth inhibition assay | TGI = 2.51 μM | 28088086 | |||
| A498 | Growth inhibition assay | GI50 = 2.51 μM | 28088086 | |||
| UACC62 | Growth inhibition assay | TGI = 2.51 μM | 28088086 | |||
| IGROV1 | Growth inhibition assay | GI50 = 2.51 μM | 28088086 | |||
| HCT15 | Growth inhibition assay | GI50 = 2.51 μM | 28088086 | |||
| SK-MEL-28 | Growth inhibition assay | GI50 = 2.51 μM | 28088086 | |||
| SK-MEL-28 | Growth inhibition assay | TGI = 2.51 μM | 28088086 | |||
| ACHN | Growth inhibition assay | GI50 = 2.51 μM | 28088086 | |||
| SK-MEL-5 | Growth inhibition assay | TGI = 2.51 μM | 28088086 | |||
| NCI/ADR-RES | Growth inhibition assay | GI50 = 2.51 μM | 28088086 | |||
| MCF7 | Growth inhibition assay | GI50 = 2.51 μM | 28088086 | |||
| SN12C | Growth inhibition assay | GI50 = 2.51 μM | 28088086 | |||
| Hs 578T | Growth inhibition assay | GI50 = 2.51 μM | 28088086 | |||
| SKOV3 | Growth inhibition assay | GI50 = 2.51 μM | 28088086 | |||
| UO31 | Growth inhibition assay | GI50 = 2.51 μM | 28088086 | |||
| NCI-H460 | Cytotoxicity assay | GI50 = 2.51 μM | 26590508 | |||
| HCT15 | Cytotoxicity assay | GI50 = 2.51 μM | 26590508 | |||
| SW620 | Cytotoxicity assay | GI50 = 2.51 μM | 26590508 | |||
| SF268 | Cytotoxicity assay | GI50 = 2.51 μM | 26590508 | |||
| IGROV1 | Cytotoxicity assay | GI50 = 2.51 μM | 26590508 | |||
| OVCAR8 | Cytotoxicity assay | GI50 = 2.51 μM | 26590508 | |||
| NCI/ADR-RES | Cytotoxicity assay | GI50 = 2.51 μM | 26590508 | |||
| SKOV3 | Cytotoxicity assay | GI50 = 2.51 μM | 26590508 | |||
| SN12C | Cytotoxicity assay | GI50 = 2.51 μM | 26590508 | |||
| NCI-H322M | Cytotoxicity assay | GI50 = 2.51 μM | 26590508 | |||
| MCF7 | Cytotoxicity assay | GI50 = 2.51 μM | 26590508 | |||
| UO31 | Cytotoxicity assay | GI50 = 2.51 μM | 26590508 | |||
| Hs578T | Cytotoxicity assay | GI50 = 2.51 μM | 26590508 | |||
| A498 | Cytotoxicity assay | GI50 = 2.51 μM | 26590508 | |||
| A498 | Antiproliferative activity assay | GI50 = 2.51 μM | 27017549 | |||
| SKOV3 | Antiproliferative activity assay | GI50 = 2.51 μM | 27017549 | |||
| UO31 | Antiproliferative activity assay | GI50 = 2.51 μM | 27017549 | |||
| NCI-ADR-RES | Antiproliferative activity assay | GI50 = 2.51 μM | 27017549 | |||
| SN12C | Antiproliferative activity assay | GI50 = 2.51 μM | 27017549 | |||
| IGROV1 | Antiproliferative activity assay | GI50 = 2.51 μM | 27017549 | |||
| ACHN | Antiproliferative activity assay | GI50 = 2.51 μM | 27017549 | |||
| OVCAR8 | Antiproliferative activity assay | GI50 = 2.51 μM | 27017549 | |||
| SK-MEL-28 | Antiproliferative activity assay | GI50 = 2.51 μM | 27017549 | |||
| NCI-H322M | Antiproliferative activity assay | GI50 = 2.51 μM | 27017549 | |||
| SF268 | Antiproliferative activity assay | GI50 = 2.51 μM | 27017549 | |||
| HCT15 | Antiproliferative activity assay | GI50 = 2.51 μM | 27017549 | |||
| NCI-H460 | Antiproliferative activity assay | GI50 = 2.51 μM | 27017549 | |||
| SW620 | Antiproliferative activity assay | GI50 = 2.51 μM | 27017549 | |||
| EKVX | Antiproliferative activity assay | GI50 = 2.51 μM | 27017549 | |||
| MCF7 | Antiproliferative activity assay | GI50 = 2.51 μM | 27017549 | |||
| Hs 578T | Antiproliferative activity assay | GI50 = 2.51 μM | 27017549 | |||
| HT-29 | Antiproliferative activity assay | IC50 = 2.58 μM | 29886324 | |||
| A375P | Antiproliferative activity assay | GI50 = 2.58 μM | 26810260 | |||
| TPC1 | Antiproliferative activity assay | EC50 = 2.6 μM | 22559926 | |||
| Hep3B | Growth inhibition assay | IC50 = 2.63 μM | 29102175 | |||
| A375P | Antiproliferative activity assay | IC50 = 2.7 μM | 22460030 | |||
| U937 | Antiproliferative activity assay | GI50 = 2.74 μM | 26318067 | |||
| U937 | Cytotoxicity assay | GI50 = 2.74 μM | 24878193 | |||
| MCF7 | Growth inhibition assay | IC50 = 2.78 μM | 29102175 | |||
| MDA-MB-231 | Antiproliferative activity assay | IC50 = 2.8 μM | 29202403 | |||
| HepG2 | Antiproliferative activity assay | IC50 = 2.84 μM | 28242553 | |||
| U937 | Growth inhibition assay | GI50 = 2.85 μM | 22014755 | |||
| A549 | Cytotoxicity assay | IC50 = 2.92 μM | 28927801 | |||
| A549 | Cytotoxicity assay | IC50 = 2.92 μM | 27777009 | |||
| ZR75-30 | Growth inhibition assay | IC50 = 2.96 μM | 29102175 | |||
| PC3 | Cytotoxicity assay | IC50 = 3.03 μM | 28340913 | |||
| MDA-MB-231 | Antiproliferative activity assay | IC50 = 3.08 μM | 26991938 | |||
| A549 | Growth inhibition assay | IC50 = 3.1 μM | 29102175 | |||
| K562 | Growth inhibition assay | GI50 = 3.16 μM | 28088086 | |||
| MOLT4 | Growth inhibition assay | GI50 = 3.16 μM | 28088086 | |||
| A549/ATCC | Growth inhibition assay | GI50 = 3.16 μM | 28088086 | |||
| RPMI8226 | Growth inhibition assay | TGI = 3.16 μM | 28088086 | |||
| SR | Growth inhibition assay | GI50 = 3.16 μM | 28088086 | |||
| HOP62 | Growth inhibition assay | TGI = 3.16 μM | 28088086 | |||
| NCI-H226 | Growth inhibition assay | TGI = 3.16 μM | 28088086 | |||
| U251 | Growth inhibition assay | TGI = 3.16 μM | 28088086 | |||
| COLO205 | Growth inhibition assay | TGI = 3.16 μM | 28088086 | |||
| M14 | Growth inhibition assay | TGI = 3.16 μM | 28088086 | |||
| HCC2998 | Growth inhibition assay | GI50 = 3.16 μM | 28088086 | |||
| SNB75 | Growth inhibition assay | GI50 = 3.16 μM | 28088086 | |||
| 786-0 | Growth inhibition assay | GI50 = 3.16 μM | 28088086 | |||
| A498 | Growth inhibition assay | TGI = 3.16 μM | 28088086 | |||
| HCT15 | Growth inhibition assay | TGI = 3.16 μM | 28088086 | |||
| OVCAR3 | Growth inhibition assay | GI50 = 3.16 μM | 28088086 | |||
| OVCAR4 | Growth inhibition assay | GI50 = 3.16 μM | 28088086 | |||
| Caki1 | Growth inhibition assay | GI50 = 3.16 μM | 28088086 | |||
| SNB19 | Growth inhibition assay | GI50 = 3.16 μM | 28088086 | |||
| OVCAR5 | Growth inhibition assay | GI50 = 3.16 μM | 28088086 | |||
| DU145 | Growth inhibition assay | GI50 = 3.16 μM | 28088086 | |||
| OVCAR8 | Growth inhibition assay | GI50 = 3.16 μM | 28088086 | |||
| SN12C | Growth inhibition assay | TGI = 3.16 μM | 28088086 | |||
| MDA-MB-231 | Growth inhibition assay | TGI = 3.16 μM | 28088086 | |||
| RXF393 | Growth inhibition assay | GI50 = 3.16 μM | 28088086 | |||
| BT549 | Growth inhibition assay | GI50 = 3.16 μM | 28088086 | |||
| K562 | Cytotoxicity assay | GI50 = 3.16 μM | 26590508 | |||
| MOLT4 | Cytotoxicity assay | GI50 = 3.16 μM | 26590508 | |||
| SNB19 | Cytotoxicity assay | GI50 = 3.16 μM | 26590508 | |||
| SR | Cytotoxicity assay | GI50 = 3.16 μM | 26590508 | |||
| A549 | Cytotoxicity assay | GI50 = 3.16 μM | 26590508 | |||
| OVCAR3 | Cytotoxicity assay | GI50 = 3.16 μM | 26590508 | |||
| OVCAR4 | Cytotoxicity assay | GI50 = 3.16 μM | 26590508 | |||
| SNB75 | Cytotoxicity assay | GI50 = 3.16 μM | 26590508 | |||
| OVCAR5 | Cytotoxicity assay | GI50 = 3.16 μM | 26590508 | |||
| DU145 | Cytotoxicity assay | GI50 = 3.16 μM | 26590508 | |||
| 786-0 | Cytotoxicity assay | GI50 = 3.16 μM | 26590508 | |||
| BT549 | Cytotoxicity assay | GI50 = 3.16 μM | 26590508 | |||
| ACHN | Cytotoxicity assay | GI50 = 3.16 μM | 26590508 | |||
| Caki1 | Cytotoxicity assay | GI50 = 3.16 μM | 26590508 | |||
| 786-0 | Antiproliferative activity assay | GI50 = 3.16 μM | 27017549 | |||
| LOXIMVI | Antiproliferative activity assay | TGI = 3.16 μM | 27017549 | |||
| Caki1 | Antiproliferative activity assay | GI50 = 3.16 μM | 27017549 | |||
| OVCAR5 | Antiproliferative activity assay | GI50 = 3.16 μM | 27017549 | |||
| RXF393 | Antiproliferative activity assay | GI50 = 3.16 μM | 27017549 | |||
| SNB75 | Antiproliferative activity assay | GI50 = 3.16 μM | 27017549 | |||
| OVCAR3 | Antiproliferative activity assay | GI50 = 3.16 μM | 27017549 | |||
| SNB19 | Antiproliferative activity assay | GI50 = 3.16 μM | 27017549 | |||
| SK-MEL-5 | Antiproliferative activity assay | TGI = 3.16 μM | 27017549 | |||
| OVCAR4 | Antiproliferative activity assay | GI50 = 3.16 μM | 27017549 | |||
| SK-MEL-2 | Antiproliferative activity assay | TGI = 3.16 μM | 27017549 | |||
| BT549 | Antiproliferative activity assay | GI50 = 3.16 μM | 27017549 | |||
| MOLT4 | Antiproliferative activity assay | GI50 = 3.16 μM | 27017549 | |||
| K562 | Antiproliferative activity assay | GI50 = 3.16 μM | 27017549 | |||
| HCC2998 | Antiproliferative activity assay | GI50 = 3.16 μM | 27017549 | |||
| HCC2998 | Antiproliferative activity assay | TGI = 3.16 μM | 27017549 | |||
| A549/ATCC | Antiproliferative activity assay | GI50 = 3.16 μM | 27017549 | |||
| DU145 | Antiproliferative activity assay | GI50 = 3.16 μM | 27017549 | |||
| SR | Antiproliferative activity assay | GI50 = 3.16 μM | 27017549 | |||
| MCF7 | Cytotoxicity assay | IC50 = 3.18 μM | 28927801 | |||
| PC3 | Cytotoxicity assay | IC50 = 3.18 μM | 28927801 | |||
| MCF7 | Cytotoxicity assay | IC50 = 3.18 μM | 27777009 | |||
| A549 | Antiproliferative activity assay | IC50 = 3.19 μM | 25778995 | |||
| PC3 | Cytotoxicity assay | IC50 = 3.24 μM | 27777009 | |||
| HeLa | Function assay | IC50 = 3.3 μM | 15225706 | |||
| HeLa | Function assay | IC50 = 3.3 μM | 15225706 | |||
| LoVo | Cytotoxicity assay | IC50 = 3.3 μM | 23454017 | |||
| A375 | Antiproliferative activity assay | IC50 = 3.36 μM | 29602674 | |||
| HT-29 | Antiproliferative activity assay | IC50 = 3.37 μM | 26991938 | |||
| FLT3 gene-deficient U937 | Antiproliferative activity assay | GI50 = 3.4 μM | 21708468 | |||
| FLT3 negative U937 | Cytotoxicity assay | GI50 = 3.4 μM | 23618709 | |||
| U937 | Cytotoxicity assay | GI50 = 3.4 μM | 26081023 | |||
| A375P | Antiproliferative activity assay | GI50 = 3.4 μM | 29459144 | |||
| ACHN | Cytotoxicity assay | IC50 = 3.4 μM | 29517908 | |||
| ACHN | Cytotoxicity assay | IC50 = 3.4 μM | 29297688 | |||
| HepG2 | Function assay | IC50 = 3.4 μM | 26071861 | |||
| A375P | Cytotoxicity assay | GI50 = 3.4 μM | 24878193 | |||
| HepG2 | Cytotoxicity assay | IC50 = 3.44 μM | 28927801 | |||
| HepG2 | Cytotoxicity assay | IC50 = 3.44 μM | 27777009 | |||
| ACHN | Cytotoxicity assay | IC50 = 3.5 μM | 29786436 | |||
| HepG2 | Antiproliferative activity assay | IC50 = 3.5 μM | 25462265 | |||
| HT-29 | Cytotoxicity assay | IC50 = 3.61 μM | 24826815 | |||
| HT-29 | Antiproliferative activity assay | IC50 = 3.61 μM | 30216849 | |||
| HT-29 | Cytotoxicity assay | IC50 = 3.61 μM | 25086238 | |||
| HT-29 | Cytotoxicity assay | IC50 = 3.61 μM | 25440879 | |||
| MCF7 | Anticancer activity assay | IC50 = 3.64 μM | 29549841 | |||
| Sf9 | Function assay | IC50 = 3.8 μM | 21708468 | |||
| Sf9 | Function assay | IC50 = 3.8 μM | 23618709 | |||
| Sf9 | Function assay | IC50 = 3.8 μM | 26081023 | |||
| A2058 | Cytotoxicity assay | IC50 = 3.8 μM | 22708987 | |||
| NCI-H460 | Cytotoxicity assay | IC50 = 3.9 μM | 23454017 | |||
| SK-MEL-30 | Cytotoxicity assay | IC50 = 3.9 μM | 29461827 | |||
| HT-29 | Anticancer activity assay | IC50 = 3.97 μM | 29549841 | |||
| SF268 | Growth inhibition assay | TGI = 3.98 μM | 28088086 | |||
| SNB75 | Growth inhibition assay | TGI = 3.98 μM | 28088086 | |||
| OVCAR3 | Growth inhibition assay | TGI = 3.98 μM | 28088086 | |||
| SNB19 | Growth inhibition assay | TGI = 3.98 μM | 28088086 | |||
| Hs 578T | Growth inhibition assay | TGI = 3.98 μM | 28088086 | |||
| TK10 | Growth inhibition assay | GI50 = 3.98 μM | 28088086 | |||
| BT549 | Growth inhibition assay | TGI = 3.98 μM | 28088086 | |||
| Caki1 | Antiproliferative activity assay | TGI = 3.98 μM | 27017549 | |||
| TK10 | Antiproliferative activity assay | GI50 = 3.98 μM | 27017549 | |||
| MDA-MB-435 | Antiproliferative activity assay | TGI = 3.98 μM | 27017549 | |||
| HCT116 | Antiproliferative activity assay | TGI = 3.98 μM | 27017549 | |||
| MDA-MB-231 | Antiproliferative activity assay | TGI = 3.98 μM | 27017549 | |||
| HepG2 | Cytotoxicity assay | IC50 = 4 μM | 23454017 | |||
| HT-29 | Cytotoxicity assay | IC50 = 4 μM | 23454017 | |||
| A549 | Cytotoxicity assay | IC50 = 4 μM | 23454017 | |||
| HuH7 | Cytotoxicity assay | GI50 = 4 μM | 23726028 | |||
| PC3 | Antiproliferative activity assay | IC50 = 4.13 μM | 25778995 | |||
| HeLa | Cytotoxicity assay | IC50 = 4.163 μM | 23362959 | |||
| MDA-MB-436 | Antiproliferative activity assay | IC50 = 4.2 μM | 29202403 | |||
| MCF7 | Cytotoxicity assay | IC50 = 4.21 μM | 27043268 | |||
| MCF7 | Cytotoxicity assay | IC50 = 4.21 μM | 28340913 | |||
| LOXIMVI | Antiproliferative activity assay | IC50 = 4.25 μM | 25778995 | |||
| OVCAR4 | Cytotoxicity assay | TGI = 4.31 μM | 26590508 | |||
| WM1361 | Antiproliferative activity assay | GI50 = 4.345 μM | 20148563 | |||
| WM266.4 | Growth inhibition assay | GI50 = 4.5 μM | 20199087 | |||
| HepG2 | Cytotoxicity assay | GI50 = 4.5 μM | 23726028 | |||
| A549 | Antiproliferative activity assay | IC50 = 4.5 μM | 23260578 | |||
| LS174T | Function assay | IC50 = 4.52 μM | 29266937 | |||
| 8505C | Antiproliferative activity assay | IC50 = 4.7 μM | 29032031 | |||
| OVCAR8 | Cytotoxicity assay | TGI = 4.73 μM | 26590508 | |||
| MDA-MB-231 | Cytotoxicity assay | IC50 = 4.77 μM | 20435479 | |||
| B16-F1 | Antiproliferative activity assay | IC50 = 4.9 μM | 18477505 | |||
| WM164 | Antiproliferative activity assay | IC50 = 4.9 μM | 17561392 | |||
| B16-F1 | Antiproliferative activity assay | IC50 = 4.9 μM | 20056548 | |||
| MDA-MB-468 | Cytotoxicity assay | IC50 = 4.9 μM | 26159483 | |||
| 786-O | Cytotoxicity assay | IC50 = 4.9 μM | 29517908 | |||
| 786-O | Cytotoxicity assay | IC50 = 4.9 μM | 29297688 | |||
| WM266.4 | Antiproliferative activity assay | GI50 = 4.933 μM | 20148563 | |||
| WM266.4 | Growth inhibition assay | IC50 = 5 μM | 19323560 | |||
| WM164 | Antiproliferative activity assay | IC50 = 5 μM | 20056548 | |||
| HepG2 | Antiproliferative activity assay | IC50 = 5 μM | 23260578 | |||
| HepG2 | Antiproliferative activity assay | IC50 = 5 μM | 23932071 | |||
| NCI-H23 | Growth inhibition assay | TGI = 5.01 μM | 28088086 | |||
| NCI-H322M | Growth inhibition assay | TGI = 5.01 μM | 28088086 | |||
| NCI-H460 | Growth inhibition assay | TGI = 5.01 μM | 28088086 | |||
| NCI-H522 | Growth inhibition assay | TGI = 5.01 μM | 28088086 | |||
| HT-29 | Growth inhibition assay | TGI = 5.01 μM | 28088086 | |||
| CCRF-CEM | Growth inhibition assay | TGI = 5.01 μM | 28088086 | |||
| SW620 | Growth inhibition assay | TGI = 5.01 μM | 28088086 | |||
| HOP92 | Growth inhibition assay | TGI = 5.01 μM | 28088086 | |||
| 786-0 | Growth inhibition assay | TGI = 5.01 μM | 28088086 | |||
| MDA-MB-435 | Growth inhibition assay | TGI = 5.01 μM | 28088086 | |||
| PC3 | Growth inhibition assay | TGI = 5.01 μM | 28088086 | |||
| UACC257 | Growth inhibition assay | TGI = 5.01 μM | 28088086 | |||
| SKOV3 | Growth inhibition assay | TGI = 5.01 μM | 28088086 | |||
| RXF393 | Growth inhibition assay | TGI = 5.01 μM | 28088086 | |||
| T47D | Growth inhibition assay | TGI = 5.01 μM | 28088086 | |||
| MDA-MB-468 | Growth inhibition assay | TGI = 5.01 μM | 28088086 | |||
| UACC62 | Antiproliferative activity assay | TGI = 5.01 μM | 27017549 | |||
| UACC257 | Antiproliferative activity assay | TGI = 5.01 μM | 27017549 | |||
| SK-MEL-5 | Antiproliferative activity assay | LC50 = 5.01 μM | 27017549 | |||
| M14 | Antiproliferative activity assay | TGI = 5.01 μM | 27017549 | |||
| NCI-H23 | Antiproliferative activity assay | TGI = 5.01 μM | 27017549 | |||
| SF295 | Antiproliferative activity assay | TGI = 5.01 μM | 27017549 | |||
| HOP92 | Antiproliferative activity assay | TGI = 5.01 μM | 27017549 | |||
| BT549 | Antiproliferative activity assay | TGI = 5.01 μM | 27017549 | |||
| MDA-MB-231 | Cytotoxicity assay | IC50 = 5.1 μM | 26159483 | |||
| DU145 | Cytotoxicity assay | IC50 = 5.1 μM | 22708987 | |||
| A549 | Cytotoxicity assay | IC50 = 5.21 μM | 20181414 | |||
| HeLa | Cytotoxicity assay | IC50 = 5.23 μM | 26342867 | |||
| 786-O | Cytotoxicity assay | IC50 = 5.3 μM | 29786436 | |||
| HCT116 | Antiproliferative activity assay | GI50 = 5.4 μM | 15225706 | |||
| A375 | Antiproliferative activity assay | IC50 = 5.4 μM | 18477505 | |||
| SK-MEL-188 | Antiproliferative activity assay | IC50 = 5.4 μM | 17561392 | |||
| A375 | Antiproliferative activity assay | IC50 = 5.4 μM | 20056548 | |||
| MCF7 | Cytotoxicity assay | IC50 = 5.5 μM | 26159483 | |||
| A375 | Antiproliferative activity assay | IC50 = 5.58 μM | 19464887 | |||
| A375P | Cytotoxicity assay | IC50 = 5.58 μM | 20797858 | |||
| A375P | Antiproliferative activity assay | GI50 = 5.58 μM | 21353571 | |||
| A375P | Growth inhibition assay | GI50 = 5.58 μM | 22014755 | |||
| A375P | Growth inhibition assay | GI50 = 5.58 μM | 20149658 | |||
| A375P | Antiproliferative activity assay | GI50 = 5.58 μM | 20466542 | |||
| A375P | Antiproliferative activity assay | IC50 = 5.6 μM | 19857963 | |||
| A375P | Antiproliferative activity assay | IC50 = 5.6 μM | 21592628 | |||
| A375P | Antiproliferative activity assay | IC50 = 5.6 μM | 22033063 | |||
| A375P | Cytotoxicity assay | IC50 = 5.6 μM | 19897366 | |||
| A375P | Antiproliferative activity assay | IC50 = 5.6 μM | 22647720 | |||
| HCT116 | Cytotoxicity assay | IC50 = 5.65 μM | 24215818 | |||
| SH-SY5Y | Antiproliferative activity assay | IC50 = 5.73 μM | 24315192 | |||
| HepG2 | Cytotoxicity assay | IC50 = 5.74 μM | 25461318 | |||
| Bel7402 | Cytotoxicity assay | IC50 = 5.8 μM | 23454017 | |||
| HT-29 | Cytotoxicity assay | IC50 = 5.9 μM | 28865276 | |||
| melanoma | Growth inhibition assay | IC50 = 6.1 μM | 16392826 | |||
| K562 | Antiproliferative activity assay | GI50 = 6.2 μM | 21708468 | |||
| HepG2 | Cytotoxicity assay | IC50 = 6.2 μM | 28865276 | |||
| A549 | Anticancer activity assay | IC50 = 6.21 μM | 29549841 | |||
| SMMC7721 | Antiproliferative activity assay | IC50 = 6.23 μM | 22721924 | |||
| HepG2 | Antiproliferative activity assay | IC50 = 6.3 μM | 23932071 | |||
| SF295 | Growth inhibition assay | TGI = 6.31 μM | 28088086 | |||
| SK-MEL-2 | Growth inhibition assay | TGI = 6.31 μM | 28088086 | |||
| OVCAR5 | Growth inhibition assay | TGI = 6.31 μM | 28088086 | |||
| UO31 | Growth inhibition assay | TGI = 6.31 μM | 28088086 | |||
| A498 | Antiproliferative activity assay | TGI = 6.31 μM | 27017549 | |||
| MALME-3M | Antiproliferative activity assay | TGI = 6.31 μM | 27017549 | |||
| U251 | Antiproliferative activity assay | TGI = 6.31 μM | 27017549 | |||
| SK-MEL-2 | Antiproliferative activity assay | LC50 = 6.31 μM | 27017549 | |||
| RPMI8226 | Antiproliferative activity assay | TGI = 6.31 μM | 27017549 | |||
| HCC2998 | Antiproliferative activity assay | LC50 = 6.31 μM | 27017549 | |||
| NCI-H522 | Antiproliferative activity assay | TGI = 6.31 μM | 27017549 | |||
| HUVEC | Antiproliferative activity assay | IC50 = 6.42 μM | 23644219 | |||
| A549 | Cytotoxicity assay | IC50 = 6.53 μM | 27043268 | |||
| A549 | Cytotoxicity assay | IC50 = 6.53 μM | 28340913 | |||
| LoVo | Antiproliferative activity assay | IC50 = 6.56 μM | 24315192 | |||
| A375 | Function assay | IC50 = 6.599 μM | 21807507 | |||
| HCT116 | Function assay | GI50 = 6.6 μM | 15225706 | |||
| HepG2 | Cytotoxicity assay | IC50 = 6.7 μM | 26159483 | |||
| BCPAP | Antiproliferative activity assay | IC50 = 6.7 μM | 29032031 | |||
| A549 | Cytotoxicity assay | IC50 = 6.7 μM | 28865276 | |||
| PC3 | Cytotoxicity assay | IC50 = 6.8 μM | 23021967 | |||
| SGC7901 | Cytotoxicity assay | IC50 = 6.9 μM | 23454017 | |||
| OS-RC2 | Cytotoxicity assay | IC50 = 7 μM | 29517908 | |||
| OS-RC2 | Cytotoxicity assay | IC50 = 7 μM | 29297688 | |||
| COLO205 | Antiproliferative activity human | IC50 = 7.04 μM | 28242553 | |||
| rhabdomyosarcoma | Cytotoxicity activity against human | CC50 = 7.05 μM | 27288186 | |||
| HuH7 | Cytotoxicity assay | IC50 = 7.1 μM | 26159483 | |||
| MDA-MB-231 | Antiproliferative activity assay | IC50 = 7.18 μM | 22721924 | |||
| FLT3-negative K562 | Cytotoxicity assay | GI50 = 7.3 μM | 23618709 | |||
| K562 | Function assay | GI50 = 7.3 μM | 26081023 | |||
| K562 | Function assay | GI50 = 7.3 μM | 26081023 | |||
| MCF7 | Antiproliferative activity assay | IC50 = 7.33 μM | 23644219 | |||
| A549 | Cytotoxicity assay | TGI = 7.36 μM | 26590508 | |||
| WI38 | Cytotoxicity assay | IC50 = 7.54 μM | 24826815 | |||
| A375 | Cytotoxicity assay | IC50 = 7.56 μM | 24215818 | |||
| MDA-MB-231 | Cytotoxicity assay | IC50 = 7.62 μM | 20181414 | |||
| 786-0 | Cytotoxicity assay | TGI = 7.62 μM | 26590508 | |||
| HS27 | Antiproliferative activity assay | IC50 = 7.8 μM | 19857963 | |||
| HS27 | Cytotoxicity assay | IC50 = 7.8 μM | 19897366 | |||
| HCT116 | Cytotoxicity assay | IC50 = 7.8 μM | 22483592 | |||
| HS27 | Antiproliferative activity assay | IC50 = 7.85 μM | 19464887 | |||
| HS27 | Antiproliferative activity assay | GI50 = 7.85 μM | 21353571 | |||
| A549/ATCC | Growth inhibition assay | TGI = 7.94 μM | 28088086 | |||
| DU145 | Growth inhibition assay | TGI = 7.94 μM | 28088086 | |||
| NCI/ADR-RES | Growth inhibition assay | TGI = 7.94 μM | 28088086 | |||
| MCF7 | Growth inhibition assay | TGI = 7.94 μM | 28088086 | |||
| PC3 | Antiproliferative activity assay | TGI = 7.94 μM | 27017549 | |||
| UO31 | Antiproliferative activity assay | TGI = 7.94 μM | 27017549 | |||
| NCI-ADR-RES | Antiproliferative activity assay | TGI = 7.94 μM | 27017549 | |||
| LOXIMVI | Antiproliferative activity assay | LC50 = 7.94 μM | 27017549 | |||
| SK-MEL-28 | Antiproliferative activity assay | TGI = 7.94 μM | 27017549 | |||
| KM12 | Antiproliferative activity assay | TGI = 7.94 μM | 27017549 | |||
| COLO205 | Antiproliferative activity assay | TGI = 7.94 μM | 27017549 | |||
| HT-29 | Antiproliferative activity assay | TGI = 7.94 μM | 27017549 | |||
| NCI-H226 | Antiproliferative activity assay | TGI = 7.94 μM | 27017549 | |||
| HOP62 | Antiproliferative activity assay | TGI = 7.94 μM | 27017549 | |||
| T47D | Antiproliferative activity assay | TGI = 7.94 μM | 27017549 | |||
| MDA-MB-468 | Antiproliferative activity assay | TGI = 7.94 μM | 27017549 | |||
| EKVX | Antiproliferative activity assay | TGI = 7.94 μM | 27017549 | |||
| MCF7 | Antiproliferative activity assay | TGI = 7.94 μM | 27017549 | |||
| Hs 578T | Antiproliferative activity assay | TGI = 7.94 μM | 27017549 | |||
| MGC803 | Antiproliferative activity assay | IC50 = 7.99 μM | 26560049 | |||
| HCT116 | Antiproliferative activity assay | IC50 = 8.08 μM | 24440479 | |||
| PC3 | Cytotoxicity assay | IC50 = 8.08 μM | 27043268 | |||
| HCT116 | Antiproliferative activity assay | IC50 = 8.08 μM | 23644219 | |||
| WM266.4 | Antiproliferative activity assay | GI50 = 8.1 μM | 23025996 | |||
| WM266.4 | Antiproliferative activity assay | GI50 = 8.12 μM | 22583669 | |||
| Ketr3 | Antiproliferative activity assay | IC50 = 8.27 μM | 30216849 | |||
| A375 | Antiproliferative activity assay | IC50 = 8.27 μM | 30216849 | |||
| HepG2 | Antiproliferative activity assay | IC50 = 8.27 μM | 30216849 | |||
| MX1 | Antiproliferative activity assay | IC50 = 8.27 μM | 30216849 | |||
| MX1 | Cytotoxicity assay | IC50 = 8.27 μM | 24675135 | |||
| WM266.4 | Growth inhibition assay | GI50 = 8.3 μM | 22361686 | |||
| PLC/PRF/5 | Cytotoxicity assay | IC50 = 8.3 μM | 21531053 | |||
| A375 | Antiproliferative activity assay | IC50 = 8.33 μM | 29886324 | |||
| HCT116 | Cytotoxicity assay | IC50 = 8.41 μM | 29631788 | |||
| WI38 | Cytotoxicity assay | IC50 = 8.42 μM | 26991938 | |||
| HepG2 | Cytotoxicity assay | IC50 = 8.42 μM | 27162123 | |||
| HepG2 | Cytotoxicity assay | IC50 = 8.42 μM | 23871909 | |||
| HT-29 | Antiproliferative activity assay | IC50 = 8.44 μM | 29602674 | |||
| HepG2 | Cytotoxicity assay | IC50 = 8.67 μM | 24675135 | |||
| MCF7 | Cytotoxicity assay | IC50 = 8.83 μM | 20435479 | |||
| MCF7 | Cytotoxicity assay | IC50 = 9.12 μM | 24300920 | |||
| HepG2 | Antiproliferative activity assay | IC50 = 9.14 μM | 26560049 | |||
| A375 | Cytotoxicity assay | IC50 = 9.17 μM | 24675135 | |||
| MGC803 | Antiproliferative activity assay | IC50 = 9.2 μM | 29032031 | |||
| SKOV3 | Cytotoxicity assay | IC50 = 9.25 μM | 24300920 | |||
| RS4:11 | Function assay | GI50 = 9.3 μM | 26081023 | |||
| RS4:11 | Cytotoxicity assay | GI50 = 9.3 μM | 23618709 | |||
| MIAPaCa2 | Antiproliferative activity assay | IC50 = 9.32 μM | 29032031 | |||
| PANC1 | Growth inhibition assay | IC50 = 9.32 μM | 29102175 | |||
| MHCC97H | Growth inhibition assay | IC50 = 9.32 μM | 29102175 | |||
| RS4:11 | Antiproliferative activity assay | GI50 = 9.4 μM | 21708468 | |||
| Hep3B | Cytotoxicity assay | IC50 = 9.4 μM | 28865276 | |||
| LoVo | Growth inhibition assay | IC50 = 9.47 μM | 29102175 | |||
| SMMC7721 | Antiproliferative activity assay | IC50 = 9.96 μM | 25637123 | |||
| MCF7 | Cytotoxicity assay | TGI = 9.97 μM | 26590508 | |||
| IGROV1 | Growth inhibition assay | TGI = 10 μM | 28088086 | |||
| ACHN | Growth inhibition assay | TGI = 10 μM | 28088086 | |||
| TK10 | Growth inhibition assay | TGI = 10 μM | 28088086 | |||
| 786-0 | Antiproliferative activity assay | TGI = 10 μM | 27017549 | |||
| SN12C | Antiproliferative activity assay | TGI = 10 μM | 27017549 | |||
| Caki1 | Antiproliferative activity assay | LC50 = 10 μM | 27017549 | |||
| TK10 | Antiproliferative activity assay | TGI = 10 μM | 27017549 | |||
| RXF393 | Antiproliferative activity assay | TGI = 10 μM | 27017549 | |||
| OVCAR8 | Antiproliferative activity assay | TGI = 10 μM | 27017549 | |||
| SNB75 | Antiproliferative activity assay | TGI = 10 μM | 27017549 | |||
| NCI-H322M | Antiproliferative activity assay | TGI = 10 μM | 27017549 | |||
| MDA-MB-435 | Antiproliferative activity assay | LC50 = 10 μM | 27017549 | |||
| SF539 | Antiproliferative activity assay | TGI = 10 μM | 27017549 | |||
| SF268 | Antiproliferative activity assay | TGI = 10 μM | 27017549 | |||
| NCI-H460 | Antiproliferative activity assay | TGI = 10 μM | 27017549 | |||
| DU145 | Antiproliferative activity assay | TGI = 10 μM | 27017549 | |||
| K1 | Antiproliferative activity assay | IC50 = 10.2 μM | 29032031 | |||
| Bel7402 | Cytotoxicity assay | IC50 = 10.26 μM | 21504204 | |||
| Bel7402 | Growth inhibition assay | IC50 = 10.31 μM | 29102175 | |||
| OVCAR3 | Cytotoxicity assay | TGI = 10.32 μM | 26590508 | |||
| SGC7901 | Cytotoxicity assay | IC50 = 10.37 μM | 20435479 | |||
| SNB75 | Cytotoxicity assay | TGI = 10.42 μM | 26590508 | |||
| A431 | Antiproliferative activity assay | IC50 = 10.46 μM | 29032031 | |||
| SMMC7721 | Antiproliferative activity assay | IC50 = 10.61 μM | 29032031 | |||
| GES-1 | Cytotoxicity assay | IC50 = 10.68 μM | 27162123 | |||
| H460 | Cytotoxicity assay | IC50 = 10.8 μM | 24300920 | |||
| BGC823 | Antiproliferative activity assay | IC50 = 10.91 μM | 22721924 | |||
| Hep3B | Cytotoxicity assay | IC50 = 11.2 μM | 28342400 | |||
| MCF7 | Cytotoxicity assay | IC50 = 11.34 μM | 27162123 | |||
| MCF7 | Cytotoxicity assay | IC50 = 11.34 μM | 23871909 | |||
| SK-MEL-2 | Antiproliferative activity human | IC50 = 11.35 μM | 28242553 | |||
| HepG2 | Cytotoxicity assay | IC50 = 11.49 μM | 21504204 | |||
| A375P | Antiproliferative activity assay | IC50 = 11.5 μM | 22014559 | |||
| SGC7901 | Cytotoxicity assay | IC50 = 11.5 μM | 24300920 | |||
| HeLa | Antiproliferative activity assay | IC50 = 12.01 μM | 29103873 | |||
| PANC1 | Cytotoxicity assay | IC50 = 12.3 μM | 24300920 | |||
| HepG2 | Antiproliferative activity assay | IC50 = 12.54 μM | 29032031 | |||
| A549 | Antiproliferative activity assay | IC50 = 12.54 μM | 23644219 | |||
| Caki1 | Growth inhibition assay | TGI = 12.59 μM | 28088086 | |||
| OVCAR8 | Growth inhibition assay | TGI = 12.59 μM | 28088086 | |||
| SKOV3 | Antiproliferative activity assay | TGI = 12.6 μM | 27017549 | |||
| ACHN | Antiproliferative activity assay | TGI = 12.6 μM | 27017549 | |||
| OVCAR3 | Antiproliferative activity assay | TGI = 12.6 μM | 27017549 | |||
| OVCAR4 | Antiproliferative activity assay | TGI = 12.6 μM | 27017549 | |||
| HCT15 | Antiproliferative activity assay | TGI = 12.6 μM | 27017549 | |||
| SW620 | Antiproliferative activity assay | TGI = 12.6 μM | 27017549 | |||
| A549/ATCC | Antiproliferative activity assay | TGI = 12.6 μM | 27017549 | |||
| MDA-MB-468 | Cytotoxicity assay | TGI = 13.09 μM | 26590508 | |||
| SK-MEL-28 | Cytotoxicity assay | TGI = 13.39 μM | 26590508 | |||
| A549 | Antiproliferative activity assay | IC50 = 13.64 μM | 26560049 | |||
| A375 | Antiproliferative activity human | IC50 = 13.64 μM | 28242553 | |||
| A375 | Antiproliferative activity assay | IC50 = 13.64 μM | 25462267 | |||
| K562 | Antiproliferative activity assay | IC50 = 13.85 μM | 23644219 | |||
| Hep3B | Cytotoxicity assay | IC50 = 14.08 μM | 21504204 | |||
| T47D | Cytotoxicity assay | TGI = 14.38 μM | 26590508 | |||
| NCI-H226 | Cytotoxicity assay | TGI = 14.42 μM | 26590508 | |||
| MDA-MB-231 | Antiproliferative activity assay | IC50 = 14.62 μM | 24440479 | |||
| MDA-MB-231 | Antiproliferative activity assay | IC50 = 14.62 μM | 23644219 | |||
| NCI-H522 | Cytotoxicity assay | TGI = 14.82 μM | 26590508 | |||
| SK-MEL-2 | Cytotoxicity assay | TGI = 14.85 μM | 26590508 | |||
| OS-RC2 | Cytotoxicity assay | IC50 = 15 μM | 29786436 | |||
| HepG2 | Antiproliferative activity assay | IC50 = 15 μM | 29103873 | |||
| fibroblast | Antiproliferative activity assay | IC50 = 15.1 μM | 18477505 | |||
| HT-29 | Cytotoxicity assay | IC50 = 15.2 μM | 24675135 | |||
| U87MG | Cytotoxicity assay | IC50 = 15.57 μM | 24826815 | |||
| BT549 | Antiproliferative activity assay | LC50 = 15.8 μM | 27017549 | |||
| GES-1 | Cytotoxicity assay | IC50 = 15.8 μM | 23871909 | |||
| SNB19 | Antiproliferative activity assay | TGI = 15.85 μM | 27017549 | |||
| IGROV1 | Antiproliferative activity assay | TGI = 15.9 μM | 27017549 | |||
| HCT116 | Antiproliferative activity assay | LC50 = 15.9 μM | 27017549 | |||
| OS-RC2 | Cytotoxicity assay | IC50 = 16 μM | 23454017 | |||
| A375 | Cytotoxicity assay | IC50 = 16.24 μM | 25461318 | |||
| SKOV3 | Cytotoxicity assay | TGI = 16.36 μM | 26590508 | |||
| WM1361 | Antiproliferative activity assay | IC50 = 16.44 μM | 29602674 | |||
| MKN28 | Antiproliferative activity assay | IC50 = 17 μM | 29032031 | |||
| SMMC7721 | Cytotoxicity assay | IC50 = 17.3 μM | 21504204 | |||
| UACC257 | Cytotoxicity assay | TGI = 17.33 μM | 26590508 | |||
| EAhy926 | Antiangiogenic activity assay | IC50 = 18.52 μM | 29032031 | |||
| SMMC7721 | Cytotoxicity assay | IC50 = 18.7 μM | 24300920 | |||
| Ketr3 | Cytotoxicity assay | IC50 = 18.8 μM | 24675135 | |||
| NCI-H522 | Cytotoxicity assay | IC50 = 19.26 μM | 25461318 | |||
| A549 | Cytotoxicity assay | IC50 = 19.54 μM | 27162123 | |||
| SH-SY5Y | Cytotoxicity assay | IC50 = 19.54 μM | 23871909 | |||
| MGC803 | Antiproliferative activity assay | IC50 = 19.92 μM | 29103873 | |||
| EKVX | Growth inhibition assay | TGI = 19.95 μM | 28088086 | |||
| OVCAR5 | Antiproliferative activity assay | TGI = 20 μM | 27017549 | |||
| UACC62 | Antiproliferative activity assay | LC50 = 20 μM | 27017549 | |||
| UACC257 | Antiproliferative activity assay | LC50 = 20 μM | 27017549 | |||
| MDA-MB-231 | Antiproliferative activity assay | LC50 = 20 μM | 27017549 | |||
| U87 | Cytotoxicity assay | IC50 = 21.07 μM | 20435479 | |||
| EJ | Cytotoxicity assay | IC50 = 22.9 μM | 24300920 | |||
| HCT116 | Antiproliferative activity assay | IC50 = 23.31 μM | 29602674 | |||
| HOP62 | Cytotoxicity assay | TGI = 23.55 μM | 26590508 | |||
| MDA-MB-231 | Cytotoxicity assay | TGI = 23.93 μM | 26590508 | |||
| PC3 | Antiproliferative activity assay | IC50 = 24.2 μM | 24440479 | |||
| PC3 | Antiproliferative activity assay | IC50 = 24.2 μM | 23644219 | |||
| EAhy926 | Antiproliferative activity assay | IC50 = 24.36 μM | 28068599 | |||
| EAhy926 | Anti-angiogenic activity in human | IC50 = 24.36 μM | 29102175 | |||
| U251 | Cytotoxicity assay | IC50 = 24.71 μM | 20435479 | |||
| NIH/3T3 | Antiproliferative activity assay | IC50 = 24.75 μM | 21592628 | |||
| NIH/3T3 | Antiproliferative activity assay | IC50 = 24.75 μM | 22647720 | |||
| DU145 | Cytotoxicity assay | IC50 = 24.91 μM | 27162123 | |||
| DU145 | Cytotoxicity assay | IC50 = 24.91 μM | 23871909 | |||
| U251 | Antiproliferative activity assay | LC50 = 25.1 μM | 27017549 | |||
| M14 | Antiproliferative activity assay | LC50 = 25.1 μM | 27017549 | |||
| NCI-H522 | Antiproliferative activity assay | LC50 = 25.1 μM | 27017549 | |||
| OVCAR4 | Growth inhibition assay | TGI = 25.12 μM | 28088086 | |||
| SH-SY5Y | Cytotoxicity assay | IC50 = 27.71 μM | 27162123 | |||
| A549 | Cytotoxicity assay | IC50 = 27.71 μM | 23871909 | |||
| PLC/PRF/5 | Cytotoxicity assay | IC50 = 29.9 μM | 28109948 | |||
| SK-MEL-5 | Cytotoxicity assay | TGI = 31.26 μM | 26590508 | |||
| A498 | Antiproliferative activity assay | LC50 = 31.6 μM | 27017549 | |||
| SK-MEL-28 | Antiproliferative activity assay | LC50 = 31.6 μM | 27017549 | |||
| KM12 | Antiproliferative activity assay | LC50 = 31.6 μM | 27017549 | |||
| COLO205 | Antiproliferative activity assay | LC50 = 31.6 μM | 27017549 | |||
| NCI-H226 | Antiproliferative activity assay | LC50 = 31.6 μM | 27017549 | |||
| SF295 | Antiproliferative activity assay | LC50 = 31.6 μM | 27017549 | |||
| HOP62 | Antiproliferative activity assay | LC50 = 31.6 μM | 27017549 | |||
| T47D | Antiproliferative activity assay | LC50 = 31.6 μM | 27017549 | |||
| MHCC97L | Cytotoxicity assay | IC50 = 34.41 μM | 28109948 | |||
| MDA-MB-231 | Antiproliferative activity assay | IC50 = 35 μM | 24315192 | |||
| MDA-MB-231 | Cytotoxicity assay | IC50 = 36 μM | 22483592 | |||
| B16-BL6 | Cytotoxicity assay | IC50 = 36.48 μM | 29631788 | |||
| UO31 | Antiproliferative activity assay | LC50 = 39.8 μM | 27017549 | |||
| SN12C | Antiproliferative activity assay | LC50 = 39.8 μM | 27017549 | |||
| RXF393 | Antiproliferative activity assay | LC50 = 39.8 μM | 27017549 | |||
| SNB75 | Antiproliferative activity assay | LC50 = 39.8 μM | 27017549 | |||
| SF268 | Antiproliferative activity assay | LC50 = 39.8 μM | 27017549 | |||
| NCI-H23 | Antiproliferative activity assay | LC50 = 39.8 μM | 27017549 | |||
| HT-29 | Antiproliferative activity assay | LC50 = 39.8 μM | 27017549 | |||
| HOP92 | Antiproliferative activity assay | LC50 = 39.8 μM | 27017549 | |||
| NCI-H460 | Antiproliferative activity assay | LC50 = 39.8 μM | 27017549 | |||
| SW620 | Antiproliferative activity assay | LC50 = 39.8 μM | 27017549 | |||
| MDA-MB-468 | Antiproliferative activity assay | LC50 = 39.8 μM | 27017549 | |||
| MALME-3M | Growth inhibition assay | TGI = 39.81 μM | 28088086 | |||
| Cliquez pour voir plus de données expérimentales sur la lignée cellulaire | ||||||
Informations chimiques, stockage et stabilité
| Poids moléculaire | 464.82 | Formule | C21H16ClF3N4O3 |
Stockage (À compter de la date de réception) | |
|---|---|---|---|---|---|
| N° CAS | 284461-73-0 | Télécharger le SDF | Stockage des solutions mères |
|
|
| Synonymes | NSC-724772,BAY 43-9006 | Smiles | CNC(=O)C1=NC=CC(=C1)OC2=CC=C(C=C2)NC(=O)NC3=CC(=C(C=C3)Cl)C(F)(F)F | ||
Solubilité
|
In vitro |
DMSO
: 92 mg/mL
(197.92 mM)
Water : Insoluble Ethanol : Insoluble |
Calculateur de molarité
Calculateur de dilution
Calculateur de poids moléculaire
|
In vivo |
|||||
Calculateur de formulation in vivo (Solution claire)
Étape 1 : Saisir les informations ci-dessous (Recommandé : Un animal supplémentaire pour tenir compte des pertes pendant lexpérience)
mg/kg
g
μL
Étape 2 : Saisir la formulation in vivo (Ceci est seulement le calculateur, pas la formulation. Veuillez nous contacter dabord sil ny a pas de formulation in vivo dans la section Solubilité.)
% DMSO
%
% Tween 80
% ddH2O
%DMSO
%
Résultats du calcul :
Concentration de travail : mg/ml;
Méthode de préparation du liquide maître DMSO : mg médicament prédissous dans μL DMSO ( Concentration du liquide maître mg/mL, Veuillez nous contacter dabord si la concentration dépasse la solubilité du DMSO du lot de médicament. )
Méthode de préparation de la formulation in vivo : Prendre μL DMSO liquide maître, puis ajouterμL PEG300, mélanger et clarifier, puis ajouterμL Tween 80, mélanger et clarifier, puis ajouter μL ddH2O, mélanger et clarifier.
Méthode de préparation de la formulation in vivo : Prendre μL DMSO liquide maître, puis ajouter μL Huile de maïs, mélanger et clarifier.
Note : 1. Veuillez vous assurer que le liquide est clair avant dajouter le solvant suivant.
2. Assurez-vous dajouter le(s) solvant(s) dans lordre. Vous devez vous assurer que la solution obtenue, lors de lajout précédent, est une solution claire avant de procéder à lajout du solvant suivant. Des méthodes physiques telles que le vortex, les ultrasons ou le bain-marie chaud peuvent être utilisées pour faciliter la dissolution.
Mécanisme daction
| Targets/IC50/Ki |
Raf-1
(Cell-free assay) 6 nM
mVEGFR2(Flk1)
(Cell-free assay) 15 nM
mVEGFR3
(Cell-free assay) 20 nM
B-Raf
(Cell-free assay) 22 nM
B-Raf (V599E)
(Cell-free assay) 38 nM
mPDGFRβ
(Cell-free assay) 57 nM
FLT3
(Cell-free assay) 58 nM
c-Kit
(Cell-free assay) 68 nM
VEGFR2
(Cell-free assay) 90 nM
FGFR1
(Cell-free assay) 580 nM
|
|---|---|
| In vitro |
Sorafenib inhibe l'activité B-Raf de type sauvage et mutante V599E avec une IC50 de 22 nM et 38 nM, respectivement. Ce composé inhibe également puissamment mVEGFR2 (Flk-1), mVEGFR3, mPDGFRβ, Flt3 et c-Kit avec une IC50 de 15 nM, 20 nM, 57 nM, 58 nM et 68 nM, respectivement. Il inhibe faiblement FGFR-1 avec une IC50 de 580 nM. Cette substance chimique n'est pas active contre ERK-1, MEK-1, EGFR, HER-2, IGFR-1, c-Met, PKB, PKA, cdk1/cyclinB, PKCα, PKCγ et pim-1. Il inhibe nettement la phosphorylation de VEGFR2 dans les cellules NIH 3T3 avec une IC50 de 30 nM et la phosphorylation de Flt-3 dans les cellules HEK-293 avec une IC50 de 20 nM. Cet agent bloque puissamment la phosphorylation de MEK 1/2 et ERK 1/2 dans la plupart des lignées cellulaires mais pas dans les cellules A549 ou H460, tout en n'ayant aucun effet sur l'inhibition de la voie PKB. Il inhibe la prolifération des cellules HAoSMC et MDA-MB-231 avec une IC50 de 0,28 μM et 2,6 μM, respectivement. En plus de l'inhibition de la voie de signalisation RAF/MEK/ERK, ce composé inhibe significativement la phosphorylation de eIF4E et régule à la baisse les niveaux de Mcl-1 dans les cellules de carcinome hépatocellulaire (HCC) d'une manière indépendante de MEK/ERK. Il inhibe la prolifération des cellules PLC/PRF/5 et HepG2 avec une IC50 de 6,3 μM et 4,5 μM, respectivement, et conduit à une induction significative de l'apoptosis.
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| Essai kinase |
Essais biochimiques
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Les baculovirus recombinants exprimant Raf-1 (résidus 305–648) et B-Raf (résidus 409–765) sont purifiés sous forme de protéines de fusion. Le MEK-1 humain pleine longueur est généré par PCR et purifié sous forme de protéine de fusion à partir de lysats d'Escherichia coli. Le tosylate de Sorafenib est ajouté à un mélange de Raf-1 (80 ng) ou de B-Raf (80 ng) avec MEK-1 (1 μg) dans un tampon d'essai [20 mM Tris (pH 8,2), 100 mM NaCl, 5 mM MgCl2 et 0,15 % de β-mercaptoéthanol] à une concentration finale de 1 % de DMSO. L'essai de kinase Raf (volume final de 50 μL) est initié par l'ajout de 25 μL de 10 μM γ[33P]ATP (400 Ci/mol) et incubé à 32 °C pendant 25 minutes. Le MEK-1 phosphorylé est récolté par filtration sur un tapis de phosphocellulose, et 1 % d'acide phosphorique est utilisé pour éliminer la radioactivité non liée. Après séchage par chauffage micro-ondes, un compteur à plaques β est utilisé pour quantifier la radioactivité liée au filtre. Le domaine kinase du VEGFR2 humain (KDR) est exprimé et purifié à partir de lysats de Sf9. Les essais de transfert d'énergie par fluorescence résolue dans le temps pour VEGFR2 sont réalisés dans des plaques opaques à 96 puits au format de transfert d'énergie par fluorescence résolue dans le temps. Les conditions de réaction finales sont les suivantes : 1 à 10 μM d'ATP, 25 nM de poly GT-biotine, 2 nM d'anticorps phospho (p)-Tyr marqué à l'europium (PY20), 10 nM d'APC, 1 à 7 nM de domaine kinase cytoplasmique à des concentrations finales de 1 % de DMSO, 50 mM de HEPES (pH 7,5), 10 mM de MgCl2, 0,1 mM d'EDTA, 0,015 % de Brij-35, 0,1 mg/mL de BSA et 0,1 % de β-mercaptoéthanol. Les volumes de réaction sont de 100 μL et sont initiés par l'ajout d'enzyme. Les plaques sont lues à 615 et 665 nm sur un compteur multilabel Perkin-Elmer VictorV environ 1,5 à 2,0 heures après l'initiation de la réaction. Le signal est calculé comme un rapport : (665 nm/615 nM) × 10 000 pour chaque puits. Pour la génération de l'IC50, ce composé est ajouté avant l'initiation de l'enzyme. Une plaque mère 50 fois concentrée est préparée avec ce composé dilué en série au 1/3 dans une solution de 50 % de DMSO/50 % d'eau distillée. Les concentrations finales de cette substance chimique varient de 10 μM à 4,56 nM dans 1 % de DMSO.
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| In vivo |
L'administration orale de Sorafenib (~60 mg/kg) démontre une activité antitumorale à large spectre, dose-dépendante, contre une variété de modèles de xénogreffes de tumeurs humaines, y compris MDA-MB-231, Colo-205, HT-29, DLD-1, NCI-H460 et A549, sans preuve de toxicité. En association avec l'efficacité antitumorale, ce traitement composé inhibe puissamment la phosphorylation de MEK 1/2 et les niveaux de pERK 1/2 dans les xénogreffes HT-29 et MDA-MB-231 mais pas dans les xénogreffes Colo-205, et supprime significativement la surface microvasculaire (MVA) et la densité microvasculaire (MVD) dans les xénogreffes tumorales MDA MB-231, HT-29 et Colo-205. Cet agent produit une inhibition de croissance dose-dépendante des xénogreffes tumorales PLC/PRF/5 chez des souris SCID avec des TGI de 49% et 78% à 10 mg/kg et 30 mg/kg, respectivement, ce qui est cohérent avec l'inhibition de la phosphorylation de ERK et eIF4E, la réduction de la surface microvasculaire et l'induction de l'apoptosis des cellules tumorales. Il sensibilise les cellules bax-/- au TRAIL de manière dose-dépendante, par un mécanisme impliquant la régulation à la baisse de l'expression de Mcl-1 et cIAP2 médiée par NF-κB. La combinaison de ce composé (30-60 mg/kg) avec le TRAIL (5 mg/kg) montre une efficacité dramatique dans les xénogreffes tumorales HCT116 bax-/- et HT29 résistantes au TRAIL.
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Références |
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Applications
| Méthodes | Biomarqueurs | Images | PMID |
|---|---|---|---|
| Western blot | LC3-I / LC-3II / ATG5 p-STAT3 / STAT3 / Mcl-1 β-catenin / Survivin / Mcl-1 / PTMA pERK / ERK p-PKM2(y105) / PMK2 / Caspase-9 RET(pY1016) / VEGFR2(pY1214) / MEK1(pT292) / ERK(pY204) Cyclin D1 |
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23392173 |
| Growth inhibition assay | Cell viability |
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26039995 |
| Immunofluorescence | p65 cytochrome c |
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22286758 |
| ELISA | TGF-beta / CD206 Caspase-9 / Caspase-3 |
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26158762 |
Informations sur lessai clinique
(données du https://clinicaltrials.gov, mis à jour le 2024-05-22)
| Numéro NCT | Recrutement | Conditions | Promoteur/Collaborateurs | Date de début | Phases |
|---|---|---|---|---|---|
| NCT05068752 | Recruiting | Pancreas Cancer |
HonorHealth Research Institute|Bayer|Genentech Inc. |
October 28 2021 | Phase 2 |
| NCT04763408 | Active not recruiting | Carcinoma Hepatocellular |
Eisai Inc. |
April 9 2021 | -- |
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