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Réf. CatalogueS1033
| Lignées cellulaires | Type dessai | Concentration | Temps dincubation | Formulation | Description de lactivité | PMID |
|---|---|---|---|---|---|---|
| EoL-1-cell | Growth Inhibition Assay | IC50=0.000144 μM | SANGER | |||
| KU812 | Growth Inhibition Assay | IC50=0.00248 μM | SANGER | |||
| EM-2 | Growth Inhibition Assay | IC50=0.0041 μM | SANGER | |||
| LAMA-84 | Growth Inhibition Assay | IC50=0.0049 μM | SANGER | |||
| MEG-01 | Growth Inhibition Assay | IC50=0.00828 μM | SANGER | |||
| BV-173 | Growth Inhibition Assay | IC50=0.01089 μM | SANGER | |||
| KASUMI-1 | Growth Inhibition Assay | IC50=0.02413 μM | SANGER | |||
| NB7 | Growth Inhibition Assay | IC50=0.13439 μM | SANGER | |||
| BHT-101 | Growth Inhibition Assay | IC50=0.64263 μM | SANGER | |||
| CGTH-W-1 | Growth Inhibition Assay | IC50=0.6487 μM | SANGER | |||
| HMV-II | Growth Inhibition Assay | IC50=0.74874 μM | SANGER | |||
| NKM-1 | Growth Inhibition Assay | IC50=0.9015 μM | SANGER | |||
| LB2241-RCC | Growth Inhibition Assay | IC50=1.02228 μM | SANGER | |||
| NCI-H1703 | Growth Inhibition Assay | IC50=1.1887 μM | SANGER | |||
| BE-13 | Growth Inhibition Assay | IC50=1.27416 μM | SANGER | |||
| ACN | Growth Inhibition Assay | IC50=1.55077 μM | SANGER | |||
| A204 | Growth Inhibition Assay | IC50=1.57205 μM | SANGER | |||
| HOP-62 | Growth Inhibition Assay | IC50=1.82077 μM | SANGER | |||
| H9 | Growth Inhibition Assay | IC50=2.73793 μM | SANGER | |||
| HCC1806 | Growth Inhibition Assay | IC50=2.74327 μM | SANGER | |||
| NOS-1 | Growth Inhibition Assay | IC50=2.87102 μM | SANGER | |||
| RS4-11 | Growth Inhibition Assay | IC50=2.90623 μM | SANGER | |||
| JAR | Growth Inhibition Assay | IC50=2.92084 μM | SANGER | |||
| T98G | Growth Inhibition Assay | IC50=3.01313 μM | SANGER | |||
| NCI-SNU-1 | Growth Inhibition Assay | IC50=3.40092 μM | SANGER | |||
| SK-MEL-1 | Growth Inhibition Assay | IC50=3.43029 μM | SANGER | |||
| L-363 | Growth Inhibition Assay | IC50=3.61107 μM | SANGER | |||
| SW982 | Growth Inhibition Assay | IC50=3.64169 μM | SANGER | |||
| HT-1080 | Growth Inhibition Assay | IC50=3.91775 μM | SANGER | |||
| G-402 | Growth Inhibition Assay | IC50=4.31203 μM | SANGER | |||
| HOS | Growth Inhibition Assay | IC50=4.80282 μM | SANGER | |||
| SK-NEP-1 | Growth Inhibition Assay | IC50=4.83191 μM | SANGER | |||
| HAL-01 | Growth Inhibition Assay | IC50=4.88242 μM | SANGER | |||
| SBC-1 | Growth Inhibition Assay | IC50=4.90907 μM | SANGER | |||
| CTV-1 | Growth Inhibition Assay | IC50=5.48938 μM | SANGER | |||
| LCLC-103H | Growth Inhibition Assay | IC50=5.77471 μM | SANGER | |||
| RVH-421 | Growth Inhibition Assay | IC50=5.77536 μM | SANGER | |||
| K-562 | Growth Inhibition Assay | IC50=5.9036 μM | SANGER | |||
| CAL-33 | Growth Inhibition Assay | IC50=6.31359 μM | SANGER | |||
| MDA-MB-361 | Growth Inhibition Assay | IC50=6.33699 μM | SANGER | |||
| IGROV-1 | Growth Inhibition Assay | IC50=6.47191 μM | SANGER | |||
| NY | Growth Inhibition Assay | IC50=6.53599 μM | SANGER | |||
| Ramos-2G6-4C10 | Growth Inhibition Assay | IC50=6.66931 μM | SANGER | |||
| HuO9 | Growth Inhibition Assay | IC50=6.73964 μM | SANGER | |||
| MS-1 | Growth Inhibition Assay | IC50=7.11953 μM | SANGER | |||
| RPMI-8226 | Growth Inhibition Assay | IC50=7.28287 μM | SANGER | |||
| HDLM-2 | Growth Inhibition Assay | IC50=7.40149 μM | SANGER | |||
| D-566MG | Growth Inhibition Assay | IC50=7.47155 μM | SANGER | |||
| SK-MEL-24 | Growth Inhibition Assay | IC50=7.63392 μM | SANGER | |||
| COLO-679 | Growth Inhibition Assay | IC50=7.98671 μM | SANGER | |||
| EW-13 | Growth Inhibition Assay | IC50=8.32054 μM | SANGER | |||
| A388 | Growth Inhibition Assay | IC50=8.38481 μM | SANGER | |||
| UM-UC-3 | Growth Inhibition Assay | IC50=8.43956 μM | SANGER | |||
| NUGC-3 | Growth Inhibition Assay | IC50=8.53582 μM | SANGER | |||
| COLO-668 | Growth Inhibition Assay | IC50=8.59491 μM | SANGER | |||
| MOLT-4 | Growth Inhibition Assay | IC50=8.62353 μM | SANGER | |||
| D-423MG | Growth Inhibition Assay | IC50=8.83756 μM | SANGER | |||
| CTB-1 | Growth Inhibition Assay | IC50=8.87128 μM | SANGER | |||
| BCPAP | Growth Inhibition Assay | IC50=9.02562 μM | SANGER | |||
| GCT | Growth Inhibition Assay | IC50=9.09831 μM | SANGER | |||
| ACHN | Growth Inhibition Assay | IC50=9.23632 μM | SANGER | |||
| KYSE-520 | Growth Inhibition Assay | IC50=9.33482 μM | SANGER | |||
| LB771-HNC | Growth Inhibition Assay | IC50=9.76497 μM | SANGER | |||
| MLMA | Growth Inhibition Assay | IC50=10.0132 μM | SANGER | |||
| HEC-1 | Growth Inhibition Assay | IC50=10.2804 μM | SANGER | |||
| HL-60 | Growth Inhibition Assay | IC50=10.6853 μM | SANGER | |||
| A101D | Growth Inhibition Assay | IC50=10.8923 μM | SANGER | |||
| A2058 | Growth Inhibition Assay | IC50=10.9245 μM | SANGER | |||
| KARPAS-45 | Growth Inhibition Assay | IC50=11.0635 μM | SANGER | |||
| 697 | Growth Inhibition Assay | IC50=11.2101 μM | SANGER | |||
| NCI-N87 | Growth Inhibition Assay | IC50=11.7731 μM | SANGER | |||
| DSH1 | Growth Inhibition Assay | IC50=11.7953 μM | SANGER | |||
| HLE | Growth Inhibition Assay | IC50=11.8839 μM | SANGER | |||
| NCI-H720 | Growth Inhibition Assay | IC50=12.6801 μM | SANGER | |||
| EW-3 | Growth Inhibition Assay | IC50=12.9307 μM | SANGER | |||
| AGS | Growth Inhibition Assay | IC50=13.0351 μM | SANGER | |||
| ES5 | Growth Inhibition Assay | IC50=13.0512 μM | SANGER | |||
| DB | Growth Inhibition Assay | IC50=13.3256 μM | SANGER | |||
| A4-Fuk | Growth Inhibition Assay | IC50=13.4102 μM | SANGER | |||
| A427 | Growth Inhibition Assay | IC50=13.4972 μM | SANGER | |||
| MN-60 | Growth Inhibition Assay | IC50=13.5843 μM | SANGER | |||
| HCC2218 | Growth Inhibition Assay | IC50=13.5856 μM | SANGER | |||
| MV-4-11 | Growth Inhibition Assay | IC50=13.8137 μM | SANGER | |||
| GI-1 | Growth Inhibition Assay | IC50=14.1184 μM | SANGER | |||
| JVM-3 | Growth Inhibition Assay | IC50=14.2656 μM | SANGER | |||
| NCI-H2029 | Growth Inhibition Assay | IC50=14.2727 μM | SANGER | |||
| TE-12 | Growth Inhibition Assay | IC50=14.6046 μM | SANGER | |||
| WM-115 | Growth Inhibition Assay | IC50=15.5683 μM | SANGER | |||
| BB65-RCC | Growth Inhibition Assay | IC50=16.0241 μM | SANGER | |||
| NCI-H1693 | Growth Inhibition Assay | IC50=16.3802 μM | SANGER | |||
| KARPAS-299 | Growth Inhibition Assay | IC50=16.6203 μM | SANGER | |||
| UACC-257 | Growth Inhibition Assay | IC50=17.0582 μM | SANGER | |||
| RKO | Growth Inhibition Assay | IC50=17.6433 μM | SANGER | |||
| HT-29 | Growth Inhibition Assay | IC50=17.7889 μM | SANGER | |||
| ES7 | Growth Inhibition Assay | IC50=18.1122 μM | SANGER | |||
| DEL | Growth Inhibition Assay | IC50=18.3172 μM | SANGER | |||
| BT-549 | Growth Inhibition Assay | IC50=18.4092 μM | SANGER | |||
| NCI-H1755 | Growth Inhibition Assay | IC50=18.5723 μM | SANGER | |||
| HCE-T | Growth Inhibition Assay | IC50=18.8341 μM | SANGER | |||
| LU-139 | Growth Inhibition Assay | IC50=19.0458 μM | SANGER | |||
| ECC10 | Growth Inhibition Assay | IC50=19.2475 μM | SANGER | |||
| 769-P | Growth Inhibition Assay | IC50=19.6335 μM | SANGER | |||
| BALL-1 | Growth Inhibition Assay | IC50=19.6775 μM | SANGER | |||
| LXF-289 | Growth Inhibition Assay | IC50=19.8979 μM | SANGER | |||
| TYK-nu | Growth Inhibition Assay | IC50=19.9315 μM | SANGER | |||
| NCI-H630 | Growth Inhibition Assay | IC50=19.9378 μM | SANGER | |||
| EW-18 | Growth Inhibition Assay | IC50=20.3802 μM | SANGER | |||
| KYSE-150 | Growth Inhibition Assay | IC50=20.7047 μM | SANGER | |||
| LOXIMVI | Growth Inhibition Assay | IC50=20.7586 μM | SANGER | |||
| HuP-T3 | Growth Inhibition Assay | IC50=21.0852 μM | SANGER | |||
| MFE-280 | Growth Inhibition Assay | IC50=21.5679 μM | SANGER | |||
| SK-OV-3 | Growth Inhibition Assay | IC50=21.8408 μM | SANGER | |||
| QIMR-WIL | Growth Inhibition Assay | IC50=22.0478 μM | SANGER | |||
| NCI-H69 | Growth Inhibition Assay | IC50=22.4299 μM | SANGER | |||
| TE-5 | Growth Inhibition Assay | IC50=22.4965 μM | SANGER | |||
| NCI-H1993 | Growth Inhibition Assay | IC50=22.4971 μM | SANGER | |||
| NCI-H1092 | Growth Inhibition Assay | IC50=23.2843 μM | SANGER | |||
| RH-1 | Growth Inhibition Assay | IC50=23.5357 μM | SANGER | |||
| DBTRG-05MG | Growth Inhibition Assay | IC50=23.8472 μM | SANGER | |||
| Mo-T | Growth Inhibition Assay | IC50=23.9 μM | SANGER | |||
| HD-MY-Z | Growth Inhibition Assay | IC50=24.2362 μM | SANGER | |||
| NCI-H2342 | Growth Inhibition Assay | IC50=24.6767 μM | SANGER | |||
| C32 | Growth Inhibition Assay | IC50=24.9576 μM | SANGER | |||
| HTC-C3 | Growth Inhibition Assay | IC50=25.3577 μM | SANGER | |||
| NCI-H358 | Growth Inhibition Assay | IC50=25.3943 μM | SANGER | |||
| CAL-85-1 | Growth Inhibition Assay | IC50=25.4577 μM | SANGER | |||
| HT-1197 | Growth Inhibition Assay | IC50=25.5319 μM | SANGER | |||
| A172 | Growth Inhibition Assay | IC50=25.7136 μM | SANGER | |||
| SW1573 | Growth Inhibition Assay | IC50=25.7785 μM | SANGER | |||
| EW-24 | Growth Inhibition Assay | IC50=25.962 μM | SANGER | |||
| SK-MEL-2 | Growth Inhibition Assay | IC50=26.0312 μM | SANGER | |||
| LU-65 | Growth Inhibition Assay | IC50=26.0452 μM | SANGER | |||
| KMOE-2 | Growth Inhibition Assay | IC50=26.0915 μM | SANGER | |||
| H-EMC-SS | Growth Inhibition Assay | IC50=26.4114 μM | SANGER | |||
| H4 | Growth Inhibition Assay | IC50=26.4243 μM | SANGER | |||
| DU-4475 | Growth Inhibition Assay | IC50=27.1872 μM | SANGER | |||
| HCT-116 | Growth Inhibition Assay | IC50=27.4349 μM | SANGER | |||
| MSTO-211H | Growth Inhibition Assay | IC50=27.6255 μM | SANGER | |||
| NCI-H292 | Growth Inhibition Assay | IC50=27.9617 μM | SANGER | |||
| NCI-H446 | Growth Inhibition Assay | IC50=28.2105 μM | SANGER | |||
| NCI-H2009 | Growth Inhibition Assay | IC50=29.1431 μM | SANGER | |||
| MHH-ES-1 | Growth Inhibition Assay | IC50=29.3685 μM | SANGER | |||
| TI-73 | Growth Inhibition Assay | IC50=29.4001 μM | SANGER | |||
| NCI-H2228 | Growth Inhibition Assay | IC50=29.458 μM | SANGER | |||
| MHH-PREB-1 | Growth Inhibition Assay | IC50=29.5505 μM | SANGER | |||
| ChaGo-K-1 | Growth Inhibition Assay | IC50=29.6097 μM | SANGER | |||
| KY821 | Growth Inhibition Assay | IC50=29.6433 μM | SANGER | |||
| NCI-H209 | Growth Inhibition Assay | IC50=29.8366 μM | SANGER | |||
| NBsusSR | Growth Inhibition Assay | IC50=29.9904 μM | SANGER | |||
| NCI-H1304 | Growth Inhibition Assay | IC50=30.5716 μM | SANGER | |||
| NB14 | Growth Inhibition Assay | IC50=31.0446 μM | SANGER | |||
| HCC1419 | Growth Inhibition Assay | IC50=31.24 μM | SANGER | |||
| KG-1 | Growth Inhibition Assay | IC50=31.7429 μM | SANGER | |||
| A2780 | Growth Inhibition Assay | IC50=31.8358 μM | SANGER | |||
| NCI-H28 | Growth Inhibition Assay | IC50=31.9861 μM | SANGER | |||
| C2BBe1 | Growth Inhibition Assay | IC50=32.2634 μM | SANGER | |||
| VA-ES-BJ | Growth Inhibition Assay | IC50=32.31 μM | SANGER | |||
| SBC-5 | Growth Inhibition Assay | IC50=32.8511 μM | SANGER | |||
| OVCAR-4 | Growth Inhibition Assay | IC50=33.4848 μM | SANGER | |||
| COR-L88 | Growth Inhibition Assay | IC50=34.0741 μM | SANGER | |||
| SW954 | Growth Inhibition Assay | IC50=34.0752 μM | SANGER | |||
| COLO-684 | Growth Inhibition Assay | IC50=34.3404 μM | SANGER | |||
| HCC70 | Growth Inhibition Assay | IC50=34.9514 μM | SANGER | |||
| NCI-H1770 | Growth Inhibition Assay | IC50=34.961 μM | SANGER | |||
| NCI-H1666 | Growth Inhibition Assay | IC50=35.8253 μM | SANGER | |||
| YH-13 | Growth Inhibition Assay | IC50=35.92 μM | SANGER | |||
| DJM-1 | Growth Inhibition Assay | IC50=36.8049 μM | SANGER | |||
| KNS-62 | Growth Inhibition Assay | IC50=36.9438 μM | SANGER | |||
| SK-MEL-30 | Growth Inhibition Assay | IC50=37.8737 μM | SANGER | |||
| SJRH30 | Growth Inhibition Assay | IC50=38.7341 μM | SANGER | |||
| GP5d | Growth Inhibition Assay | IC50=38.8653 μM | SANGER | |||
| SW1116 | Growth Inhibition Assay | IC50=39.2805 μM | SANGER | |||
| COLO-800 | Growth Inhibition Assay | IC50=39.3638 μM | SANGER | |||
| RD | Growth Inhibition Assay | IC50=39.5258 μM | SANGER | |||
| NCI-SNU-5 | Growth Inhibition Assay | IC50=39.6916 μM | SANGER | |||
| HuO-3N1 | Growth Inhibition Assay | IC50=40.108 μM | SANGER | |||
| SK-UT-1 | Growth Inhibition Assay | IC50=40.5674 μM | SANGER | |||
| SK-MEL-3 | Growth Inhibition Assay | IC50=40.5932 μM | SANGER | |||
| SK-MEL-28 | Growth Inhibition Assay | IC50=40.6435 μM | SANGER | |||
| SCC-4 | Growth Inhibition Assay | IC50=41.2137 μM | SANGER | |||
| no-11 | Growth Inhibition Assay | IC50=41.7354 μM | SANGER | |||
| HT-144 | Growth Inhibition Assay | IC50=42.0567 μM | SANGER | |||
| MFM-223 | Growth Inhibition Assay | IC50=42.402 μM | SANGER | |||
| ONS-76 | Growth Inhibition Assay | IC50=42.8018 μM | SANGER | |||
| ES8 | Growth Inhibition Assay | IC50=43.3698 μM | SANGER | |||
| T-24 | Growth Inhibition Assay | IC50=43.4369 μM | SANGER | |||
| GAMG | Growth Inhibition Assay | IC50=43.4517 μM | SANGER | |||
| LU-135 | Growth Inhibition Assay | IC50=44.0923 μM | SANGER | |||
| HCC1187 | Growth Inhibition Assay | IC50=44.8262 μM | SANGER | |||
| TE-1 | Growth Inhibition Assay | IC50=45.1654 μM | SANGER | |||
| J-RT3-T3-5 | Growth Inhibition Assay | IC50=45.4315 μM | SANGER | |||
| GI-ME-N | Growth Inhibition Assay | IC50=45.8952 μM | SANGER | |||
| D-392MG | Growth Inhibition Assay | IC50=45.9256 μM | SANGER | |||
| KALS-1 | Growth Inhibition Assay | IC50=46.7257 μM | SANGER | |||
| MMAC-SF | Growth Inhibition Assay | IC50=46.9952 μM | SANGER | |||
| HSC-3 | Growth Inhibition Assay | IC50=47.3608 μM | SANGER | |||
| KM-H2 | Growth Inhibition Assay | IC50=47.6007 μM | SANGER | |||
| LoVo | Growth Inhibition Assay | IC50=48.1002 μM | SANGER | |||
| NCI-H510A | Growth Inhibition Assay | IC50=48.1871 μM | SANGER | |||
| EW-11 | Growth Inhibition Assay | IC50=48.2348 μM | SANGER | |||
| HCC2998 | Growth Inhibition Assay | IC50=48.6236 μM | SANGER | |||
| J82 | Growth Inhibition Assay | IC50=48.7242 μM | SANGER | |||
| ML-2 | Growth Inhibition Assay | IC50=49.4605 μM | SANGER | |||
| NCI-H2030 | Growth Inhibition Assay | IC50=49.7117 μM | SANGER | |||
| NCI-H1792 | Growth Inhibition Assay | IC50=49.8518 μM | SANGER | |||
| KU812 | Antiproliferative assay | 72 hrs | Antiproliferative activity against human KU812 cells assessed as cell viability after 72 hrs by CellTiter-Glo or CCK-8 assay, GI50 = 0.001 μM. | 26789553 | ||
| BA/F3 | Antiproliferative assay | 72 hrs | Antiproliferative activity against mouse BA/F3 cells expressing Bcr-Abl M244V mutant after 72 hrs by CCK-8 assay, IC50 = 0.00154 μM. | 23088644 | ||
| K562 | Antiproliferative assay | 72 hrs | Antiproliferative activity against human K562 cells assessed as cell viability after 72 hrs by CellTiter-Glo or CCK-8 assay, GI50 = 0.002 μM. | 26789553 | ||
| BA/F3 | Cytotoxicity assay | 72 hrs | Cytotoxicity against mouse BA/F3 cells expressing BCR-ABL M351T mutant assessed as growth inhibition after 72 hrs by CCK-8 assay, IC50 = 0.003 μM. | 23301703 | ||
| KU812 | Antiproliferative assay | Antiproliferative activity against human KU812 cells, IC50 = 0.0034 μM. | 21376587 | |||
| Ba/F3 | Function assay | 48 hrs | Inhibition of wild type BCR-ABL1 (unknown origin) expressed in mouse Ba/F3 cells assessed as inhibition of cell proliferation after 48 hrs by BriteLight luciferase assay, GI50 = 0.00352 μM. | 30137981 | ||
| HEK293 | Function assay | Inhibition of autophosphorylation of DDR1 expressed in HEK293 cells by ELISA, IC50 = 0.0037 μM. | 20817538 | |||
| Ba/F3 | Function assay | 48 hrs | Inhibition of BCR-ABL1 G250H mutant (unknown origin) expressed in mouse Ba/F3 cells assessed as inhibition of BCR-ABL1-mediated cell proliferation after 48 hrs by BriteLight luciferase assay, GI50 = 0.00371 μM. | 30137981 | ||
| K562 | Cytotoxicity assay | 72 hrs | Cytotoxicity against human K562 cells assessed as cell viability after 72 hrs by MTT assay, IC50 = 0.0039 μM. | 26814890 | ||
| BA/F3 | Function assay | 72 hrs | Inhibition of BCR/ABL p210 (unknown origin) expressed in mouse BA/F3 cells assessed as growth inhibition after 72 hrs by CellTiter-Glo or CCK-8 assay, GI50 = 0.004 μM. | 26789553 | ||
| Ba/F3 | Function assay | 48 hrs | Inhibition of BCR-ABL1 E355G mutant (unknown origin) expressed in mouse Ba/F3 cells assessed as inhibition of BCR-ABL1-mediated cell proliferation after 48 hrs by BriteLight luciferase assay, GI50 = 0.00482 μM. | 30137981 | ||
| HEK293 | Function assay | Inhibition of autophosphorylation of DDR2 expressed in HEK293 cells by ELISA, IC50 = 0.0052 μM. | 20817538 | |||
| BA/F3 | Antiproliferative assay | 72 hrs | Antiproliferative activity against mouse BA/F3 cells expressing Bcr-Abl H396P mutant after 72 hrs by CCK-8 assay, IC50 = 0.00634 μM. | 23088644 | ||
| K562 | Antiproliferative assay | Antiproliferative activity against human K562 cells, IC50 = 0.0065 μM. | 21376587 | |||
| BA/F3 | Antiproliferative assay | 72 hrs | Antiproliferative activity against mouse BA/F3 cells expressing Bcr-Abl E355G mutant after 72 hrs by CCK-8 assay, IC50 = 0.00838 μM. | 23088644 | ||
| Ba/F3 | Function assay | 48 hrs | Inhibition of BCR-ABL1 E459K mutant (unknown origin) expressed in mouse Ba/F3 cells assessed as inhibition of BCR-ABL1-mediated cell proliferation after 48 hrs by BriteLight luciferase assay, GI50 = 0.00921 μM. | 30137981 | ||
| BA/F3 | Cytotoxicity assay | 72 hrs | Cytotoxicity against mouse BA/F3 cells expressing BCR-ABL F486S mutant assessed as growth inhibition after 72 hrs by CCK-8 assay, IC50 = 0.0095 μM. | 23301703 | ||
| BA/F3 | Antiproliferative assay | 72 hrs | Antiproliferative activity against mouse BA/F3 cells expressing Bcr-Abl M351T mutant after 72 hrs by CCK-8 assay, IC50 = 0.0103 μM. | 23088644 | ||
| insect cells | Function assay | 30 mins | Inhibition of human recombinant ABL1 M351T mutant expressed in insect cells after 30 mins by FRET assay, IC50 = 0.0128 μM. | 23301703 | ||
| K562 | Antiproliferative assay | 72 hrs | Antiproliferative activity against human K562 cells after 72 hrs by CCK8 assay, IC50 = 0.015 μM. | 23521020 | ||
| insect cells | Function assay | 30 mins | Inhibition of human recombinant ABL1 H396P mutant expressed in insect cells after 30 mins by FRET assay, IC50 = 0.0158 μM. | 23301703 | ||
| MEG01 | Antiproliferative assay | 72 hrs | Antiproliferative activity against human MEG01 cells assessed as cell viability after 72 hrs by CellTiter-Glo or CCK-8 assay, GI50 = 0.016 μM. | 26789553 | ||
| BA/F3 | Function assay | 72 hrs | Inhibition of BCR/ABL p210-M351T mutant (unknown origin) expressed in mouse BA/F3 cells assessed as growth inhibition after 72 hrs by CellTiter-Glo or CCK-8 assay, GI50 = 0.017 μM. | 26789553 | ||
| Ba/F3 | Function assay | 48 hrs | Inhibition of BCR-ABL1 Q252H mutant (unknown origin) expressed in mouse Ba/F3 cells assessed as inhibition of BCR-ABL1-mediated cell proliferation after 48 hrs by BriteLight luciferase assay, GI50 = 0.0189 μM. | 30137981 | ||
| Ba/F | Function assay | Inhibition of autophosphorylation of BCR-ABL1 expressed in Ba/F cells, IC50 = 0.02 μM. | 20817538 | |||
| K562 | Antiproliferative assay | Antiproliferative activity against human K562 cells, IC50 = 0.021 μM. | 20817538 | |||
| BA/F3 | Antiproliferative assay | 72 hrs | Antiproliferative activity against mouse BA/F3 cells expressing Bcr-Abl F486S mutant after 72 hrs by CCK-8 assay, IC50 = 0.021 μM. | 23088644 | ||
| BA/F3 | Function assay | 72 hrs | Inhibition of BCR/ABL p210-E255K mutant (unknown origin) expressed in mouse BA/F3 cells assessed as growth inhibition after 72 hrs by CellTiter-Glo or CCK-8 assay, GI50 = 0.021 μM. | 26789553 | ||
| BA/F3 | Cytotoxicity assay | 72 hrs | Cytotoxicity against mouse BA/F3 cells expressing wild type BCR-ABL assessed as growth inhibition after 72 hrs by CCK-8 assay, IC50 = 0.022 μM. | 23301703 | ||
| K562 | Antiproliferative assay | 72 hrs | Antiproliferative activity against human K562 cells expressing wild type Bcr-Abl after 72 hrs by CCK-8 assay, IC50 = 0.022 μM. | 26195136 | ||
| BA/F3 | Function assay | 72 hrs | Inhibition of BCR/ABL p210-Q252H mutant (unknown origin) expressed in mouse BA/F3 cells assessed as growth inhibition after 72 hrs by CellTiter-Glo or CCK-8 assay, GI50 = 0.023 μM. | 26789553 | ||
| insect cells | Function assay | 30 mins | Inhibition of human recombinant ABL1 Q252H mutant expressed in insect cells after 30 mins by FRET assay, IC50 = 0.0242 μM. | 23301703 | ||
| BA/F3 | Antiproliferative assay | Antiproliferative activity against BCR-ABL1 transfected mouse BA/F3 cells, IC50 = 0.025 μM. | 20817538 | |||
| BA/F3 | Function assay | 72 hrs | Inhibition of BCR/ABL p210-H369P mutant (unknown origin) expressed in mouse BA/F3 cells assessed as growth inhibition after 72 hrs by CellTiter-Glo or CCK-8 assay, GI50 = 0.025 μM. | 26789553 | ||
| insect cells | Function assay | 30 mins | Inhibition of human recombinant ABL1 E255K mutant expressed in insect cells after 30 mins by FRET assay, IC50 = 0.0278 μM. | 23301703 | ||
| K562 | Function assay | 30 mins | Inhibition of kinobead binding to ABL in human K562 cells incubated for 30 mins by iTRAQ reagent-based mass spectrometric method, IC50 = 0.028 μM. | 28280261 | ||
| Ba/F3 | Function assay | 48 hrs | Inhibition of BCR-ABL1 F359V mutant (unknown origin) expressed in mouse Ba/F3 cells assessed as inhibition of BCR-ABL1-mediated cell proliferation after 48 hrs by BriteLight luciferase assay, GI50 = 0.0296 μM. | 30137981 | ||
| insect cells | Function assay | 30 mins | Inhibition of human recombinant ABL1 Y253F mutant expressed in insect cells after 30 mins by FRET assay, IC50 = 0.0299 μM. | 23301703 | ||
| Ba/F3 | Function assay | 48 hrs | Inhibition of BCR-ABL1 E255K mutant (unknown origin) expressed in mouse Ba/F3 cells assessed as inhibition of BCR-ABL1-mediated cell proliferation after 48 hrs by BriteLight luciferase assay, GI50 = 0.0369 μM. | 30137981 | ||
| BA/F3 | Antiproliferative assay | 72 hrs | Antiproliferative activity against mouse BA/F3 cells expressing Bcr-Abl G250E mutant after 72 hrs by CCK-8 assay, IC50 = 0.0386 μM. | 23088644 | ||
| K562 | Function assay | Inhibition of BCR-ABL1 autophosphorylation in human K562 cells, IC50 = 0.042 μM. | 20817538 | |||
| insect cells | Function assay | 30 mins | Inhibition of human recombinant wild type ABL1 expressed in insect cells after 30 mins by FRET assay, IC50 = 0.0435 μM. | 23301703 | ||
| BA/F3 | Function assay | 72 hrs | Inhibition of BCR/ABL p210-F317I mutant (unknown origin) expressed in mouse BA/F3 cells assessed as growth inhibition after 72 hrs by CellTiter-Glo or CCK-8 assay, GI50 = 0.0546 μM. | 26789553 | ||
| BA/F3 | Antiproliferative assay | 72 hrs | Antiproliferative activity against mouse BA/F3 cells expressing Bcr-Abl Y253F mutant after 72 hrs by CCK-8 assay, IC50 = 0.0607 μM. | 23088644 | ||
| Ba/F3 | Function assay | 48 hrs | Inhibition of BCR-ABL1 E255V mutant (unknown origin) expressed in mouse Ba/F3 cells assessed as inhibition of BCR-ABL1-mediated cell proliferation after 48 hrs by BriteLight luciferase assay, GI50 = 0.0616 μM. | 30137981 | ||
| BA/F3 | Antiproliferative assay | Antiproliferative activity against PDGFRbeta transfected mouse BA/F3 cells, IC50 = 0.062 μM. | 20817538 | |||
| BA/F3 | Antiproliferative assay | 72 hrs | Antiproliferative activity against mouse BA/F3 cells expressing wild type Bcr-Abl after 72 hrs by CCK-8 assay, IC50 = 0.0652 μM. | 23088644 | ||
| A31 | Function assay | Inhibition of human PDGFRalpha autophosphorylation in human A31 cells by ELISA, IC50 = 0.071 μM. | 20817538 | |||
| A31 | Function assay | Inhibition of PDGFRbeta autophosphorylation in human A31 cells by ELISA, IC50 = 0.071 μM. | 20817538 | |||
| BA/F3 | Antiproliferative assay | 72 hrs | Antiproliferative activity against mouse BA/F3 cells expressing Bcr-Abl H396R mutant after 72 hrs by CCK-8 assay, IC50 = 0.0872 μM. | 23088644 | ||
| K562 | Function assay | 30 mins | Inhibition of kinobead binding to DDR1 in human K562 cells incubated for 30 mins by iTRAQ reagent-based mass spectrometric method, IC50 = 0.1 μM. | 28280261 | ||
| BA/F3 | Cytotoxicity assay | 72 hrs | Cytotoxicity against mouse BA/F3 cells expressing BCR-ABL E359V mutant assessed as growth inhibition after 72 hrs by CCK-8 assay, IC50 = 0.12 μM. | 23301703 | ||
| BA/F3 | Cytotoxicity assay | 72 hrs | Cytotoxicity against mouse BA/F3 cells expressing BCR-ABL Q252H mutant assessed as growth inhibition after 72 hrs by CCK-8 assay, IC50 = 0.12 μM. | 23301703 | ||
| BA/F3 | Cytotoxicity assay | 72 hrs | Cytotoxicity against mouse BA/F3 cells expressing BCR-ABL E355G mutant assessed as growth inhibition after 72 hrs by CCK-8 assay, IC50 = 0.13 μM. | 23301703 | ||
| Ba/F3 | Function assay | 48 hrs | Inhibition of BCR-ABL1 Y253H mutant (unknown origin) expressed in mouse Ba/F3 cells assessed as inhibition of BCR-ABL1-mediated cell proliferation after 48 hrs by BriteLight luciferase assay, GI50 = 0.132 μM. | 30137981 | ||
| BA/F3 | Antiproliferative assay | 72 hrs | Antiproliferative activity against mouse BA/F3 cells expressing Bcr-Abl Q252H mutant after 72 hrs by CCK-8 assay, IC50 = 0.15 μM. | 23088644 | ||
| BA/F3 | Cytotoxicity assay | 72 hrs | Cytotoxicity against mouse BA/F3 cells expressing BCR-ABL G250E mutant assessed as growth inhibition after 72 hrs by CCK-8 assay, IC50 = 0.15 μM. | 23301703 | ||
| GIST882 | Antiproliferative assay | Antiproliferative activity against human GIST882 cells, IC50 = 0.151 μM. | 20817538 | |||
| BA/F3 | Antiproliferative assay | 72 hrs | Antiproliferative activity against mouse BA/F3 cells expressing Bcr-Abl F359V mutant after 72 hrs by CCK-8 assay, IC50 = 0.159 μM. | 23088644 | ||
| BA/F3 | Cytotoxicity assay | 72 hrs | Cytotoxicity against mouse BA/F3 cells expressing BCR-ABL F317L mutant assessed as growth inhibition after 72 hrs by CCK-8 assay, IC50 = 0.16 μM. | 23301703 | ||
| BA/F3 | Cytotoxicity assay | 72 hrs | Cytotoxicity against mouse BA/F3 cells expressing BCR-ABL E255K mutant assessed as growth inhibition after 72 hrs by CCK-8 assay, IC50 = 0.17 μM. | 23301703 | ||
| BA/F3 | Function assay | 72 hrs | Inhibition of BCR/ABL p210-F317L mutant (unknown origin) expressed in mouse BA/F3 cells assessed as growth inhibition after 72 hrs by CellTiter-Glo or CCK-8 assay, GI50 = 0.202 μM. | 26789553 | ||
| insect cells | Function assay | 30 mins | Inhibition of human recombinant ABL1 G250E mutant expressed in insect cells after 30 mins by FRET assay, IC50 = 0.2153 μM. | 23301703 | ||
| GIST882 | Function assay | Inhibition of human KIT autophosphorylation in human GIST882 cells by ELISA, IC50 = 0.217 μM. | 20817538 | |||
| K562 | Antiproliferative assay | Antiproliferative activity against human imatinib-resistant K562 cells, IC50 = 0.26 μM. | 21376587 | |||
| BA/F3 | Antiproliferative assay | 72 hrs | Antiproliferative activity against mouse BA/F3 cells expressing Bcr-Abl E255K mutant after 72 hrs by CCK-8 assay, IC50 = 0.292 μM. | 23088644 | ||
| BA/F3 | Antiproliferative assay | 72 hrs | Antiproliferative activity against mouse BA/F3 cells expressing Bcr-Abl Y253H mutant after 72 hrs by CCK-8 assay, IC50 = 0.314 μM. | 23088644 | ||
| BA/F3 | Function assay | 72 hrs | Inhibition of TEL-SRC (unknown origin) expressed in mouse BA/F3 cells assessed as growth inhibition after 72 hrs by CellTiter-Glo or CCK-8 assay, GI50 = 0.47 μM. | 26789553 | ||
| BA/F3 | Antiproliferative assay | 72 hrs | Antiproliferative activity against mouse BA/F3 cells expressing Bcr-Abl E255V mutant after 72 hrs by CCK-8 assay, IC50 = 0.473 μM. | 23088644 | ||
| HEK293 | Function assay | Inhibition of autophosphorylation of CSF1R expressed in HEK293 cells by ELISA, IC50 = 0.677 μM. | 20817538 | |||
| insect cells | Function assay | 30 mins | Inhibition of human recombinant ABL1 T315I mutant expressed in insect cells after 30 mins by FRET assay, IC50 = 0.7024 μM. | 23301703 | ||
| BA/F3 | Antiproliferative assay | 72 hrs | Antiproliferative activity against mouse BA/F3 cells expressing Bcr-Abl T315I mutant after 72 hrs by CCK-8 assay, IC50 = 0.775 μM. | 23088644 | ||
| M-NFS-60 | Antiproliferative assay | Antiproliferative activity against mouse M-NFS-60 cells, IC50 = 0.838 μM. | 20817538 | |||
| BA/F3 | Function assay | 72 hrs | Inhibition of TEL-LCK (unknown origin) expressed in mouse BA/F3 cells assessed as growth inhibition after 72 hrs by CellTiter-Glo or CCK-8 assay, GI50 = 0.87 μM. | 26789553 | ||
| BA/F3 | Cytotoxicity assay | 72 hrs | Cytotoxicity against mouse BA/F3 cells expressing BCR-ABL Y253H mutant assessed as growth inhibition after 72 hrs by CCK-8 assay, IC50 = 1 μM. | 23301703 | ||
| BA/F3 | Function assay | 72 hrs | Inhibition of BCR/ABL p210-Y253F mutant (unknown origin) expressed in mouse BA/F3 cells assessed as growth inhibition after 72 hrs by CellTiter-Glo or CCK-8 assay, GI50 = 1.093 μM. | 26789553 | ||
| BA/F3 | Function assay | 72 hrs | Inhibition of TEL-DDR1 (unknown origin) expressed in mouse BA/F3 cells assessed as growth inhibition after 72 hrs by CellTiter-Glo or CCK-8 assay, GI50 = 1.1 μM. | 26789553 | ||
| BA/F3 | Cytotoxicity assay | 72 hrs | Cytotoxicity against mouse BA/F3 cells expressing BCR-ABL E255V mutant assessed as growth inhibition after 72 hrs by CCK-8 assay, IC50 = 1.2 μM. | 23301703 | ||
| BA/F3 | Function assay | 72 hrs | Inhibition of TEL-BLK (unknown origin) expressed in mouse BA/F3 cells assessed as growth inhibition after 72 hrs by CellTiter-Glo or CCK-8 assay, GI50 = 1.3 μM. | 26789553 | ||
| BA/F3 | Cytotoxicity assay | 72 hrs | Cytotoxicity against mouse BA/F3 cells expressing BCR-ABL Y253F mutant assessed as growth inhibition after 72 hrs by CCK-8 assay, IC50 = 1.4 μM. | 23301703 | ||
| BA/F3 | Function assay | 72 hrs | Inhibition of TEL-DDR2 (unknown origin) expressed in mouse BA/F3 cells assessed as growth inhibition after 72 hrs by CellTiter-Glo or CCK-8 assay, GI50 = 1.4 μM. | 26789553 | ||
| NCI-H2286 | Antiproliferative assay | 72 hrs | Antiproliferative activity against human NCI-H2286 cells expressing DDR2 mutant after 72 hrs by alamar blue assay, IC50 = 1.8 μM. | 26191369 | ||
| K562 | Function assay | 30 mins | Inhibition of kinobead binding to NQO2 in human K562 cells incubated for 30 mins by iTRAQ reagent-based mass spectrometric method, IC50 = 1.8 μM. | 28280261 | ||
| BA/F3 | Antiproliferative assay | 72 hrs | Antiproliferative activity against mouse BA/F3 cells assessed as cell viability after 72 hrs by CellTiter-Glo or CCK-8 assay, GI50 = 2.1 μM. | 26789553 | ||
| Ba/F3 | Function assay | 48 hrs | Inhibition of BCR-ABL1 T315I mutant (unknown origin) expressed in mouse Ba/F3 cells assessed as inhibition of cell proliferation after 48 hrs by BriteLight luciferase assay, GI50 = 2.262 μM. | 30137981 | ||
| HCT116 | Antiproliferative assay | 72 hrs | Antiproliferative activity against human HCT116 cells after 72 hrs by MTT assay, IC50 = 2.39 μM. | 23521020 | ||
| K562 | Antiproliferative assay | 72 hrs | Antiproliferative activity against apoptosis-resistant, Philadelphia chromosome-positive human K562 cells after 72 hrs by PrestoBlue colorimetric assay, IC50 = 2.4 μM. | 24835982 | ||
| MDA-MB-435S | Antiproliferative assay | 72 hrs | Antiproliferative activity against human MDA-MB-435S cells after 72 hrs by MTT assay, IC50 = 2.66 μM. | 23521020 | ||
| BA/F3 | Cytotoxicity assay | 72 hrs | Cytotoxicity against mouse BA/F3 cells expressing BCR-ABL T315I mutant after 72 hrs by MTT assay, IC50 = 2.7 μM. | 26814890 | ||
| BA/F3 | Cytotoxicity assay | 72 hrs | Cytotoxicity against mouse BA/F3 cells expressing BCR-ABL F317V mutant assessed as growth inhibition after 72 hrs by CCK-8 assay, IC50 = 2.9 μM. | 23301703 | ||
| BA/F3 | Cytotoxicity assay | 72 hrs | Cytotoxicity against mouse BA/F3 cells expressing BCR-ABL L248V mutant assessed as growth inhibition after 72 hrs by CCK-8 assay, IC50 = 3 μM. | 23301703 | ||
| NCI-H23 | Antiproliferative assay | 72 hrs | Antiproliferative activity against human NCI-H23 cells after 72 hrs by MTT assay, IC50 = 3.05 μM. | 23521020 | ||
| HEL | Antiproliferative assay | 72 hrs | Antiproliferative activity against human HEL cells assessed as cell viability after 72 hrs by CellTiter-Glo or CCK-8 assay, GI50 = 3.9 μM. | 26789553 | ||
| BA/F3 | Function assay | 72 hrs | Inhibition of TEL-HCK (unknown origin) expressed in mouse BA/F3 cells assessed as growth inhibition after 72 hrs by CellTiter-Glo or CCK-8 assay, GI50 = 4.1 μM. | 26789553 | ||
| CHL | Antiproliferative assay | 72 hrs | Antiproliferative activity against human CHL cells assessed as cell viability after 72 hrs by CellTiter-Glo or CCK-8 assay, GI50 = 4.2 μM. | 26789553 | ||
| CHO | Function assay | Inhibition of Cav1.2 current measured using QPatch automatic path clamp system in CHO cells expressing Cav1.2, beta-2 and alpha-2/delta-1 subunits, IC50 = 4.7 μM. | 23812503 | |||
| T47D | Antiproliferative assay | 72 hrs | Antiproliferative activity against human T47D cells after 72 hrs by MTT assay, IC50 = 6.08 μM. | 23521020 | ||
| A549 | Antiproliferative assay | 72 hrs | Antiproliferative activity against human A549 cells after 72 hrs by MTT assay, IC50 = 6.63 μM. | 23521020 | ||
| MCF7 | Antiproliferative assay | 72 hrs | Antiproliferative activity against human MCF7 cells after 72 hrs by MTT assay, IC50 = 6.92 μM. | 23521020 | ||
| BJ | Antiproliferative assay | 72 hrs | Antiproliferative activity against human BJ cells after 72 hrs by PrestoBlue colorimetric assay, IC50 = 12.8 μM. | 24835982 | ||
| NCI-H460 | Antiproliferative assay | 72 hrs | Antiproliferative activity against human NCI-H460 cells after 72 hrs by MTT assay, IC50 = 14.41 μM. | 23521020 | ||
| BA/F3 | Cytotoxicity assay | 72 hrs | Cytotoxicity against mouse BA/F3 cells assessed as growth inhibition after 72 hrs by CCK-8 assay, IC50 = 15.1 μM. | 23301703 | ||
| BA/F3 | Cytotoxicity assay | 72 hrs | Cytotoxicity against mouse BA/F3 cells expressing BCR-ABL T315I mutant assessed as growth inhibition after 72 hrs by CCK-8 assay, IC50 = 16 μM. | 23301703 | ||
| BA/F3 | Cytotoxicity assay | 72 hrs | Cytotoxicity against mouse BA/F3 cells expressing BCR-ABL H396R mutant assessed as growth inhibition after 72 hrs by CCK-8 assay, IC50 = 21.1 μM. | 23301703 | ||
| BA/F3 | Antiproliferative assay | 72 hrs | Antiproliferative activity against mouse BA/F3 cells after 72 hrs by CCK-8 assay, IC50 = 40.75 μM. | 23088644 | ||
| BA/F3 | Antitumor assay | 75 mg/kg | 19 days | Antitumor activity against mouse BA/F3 cells expressing wild type Bcr-Abl xenografted in CB17 SCID mouse assessed as median survival time at 75 mg/kg, po administered on day 3 once daily for 19 days relative to control | 19572547 | |
| BA/F3 | Antitumor assay | 75 mg/kg | 19 days | Antitumor activity against mouse BA/F3 cells expressing wild type Bcr-Abl xenografted in CB17 SCID mouse assessed as increase in mouse survival at 75 mg/kg, po administered on day 3 once daily for 19 days relative to control | 19572547 | |
| vascular smooth muscle cells | Antiangiogenic assay | 0.15 uM | 72 hrs | Antiangiogenic activity in HUVEC co-cultured with vascular smooth muscle cells assessed as inhibition of cell growth at 0.15 uM after 72 hrs | 22853993 | |
| vascular smooth muscle cells | Antiangiogenic assay | 10 to 15 uM | 72 hrs | Antiangiogenic activity in HUVEC co-cultured with vascular smooth muscle cells assessed as inhibition of network formation at 10 to 15 uM after 72 hrs | 22853993 | |
| HEK293 | Function assay | 0.1 to 1 uM | 16 hrs | Inhibition of collagen I-induced DDR2 (unknown origin) phosphorylation expressed in HEK293 cells at 0.1 to 1 uM after 16 hrs by Western blotting | 26191369 | |
| HEK293 | Function assay | 0.1 to 1 uM | 16 hrs | Inhibition of collagen I-induced DDR2 I638F mutant (unknown origin) phosphorylation expressed in HEK293 cells at 0.1 to 1 uM after 16 hrs by Western blotting | 26191369 | |
| SJ-GBM2 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SJ-GBM2 cells | 29435139 | |||
| NB-EBc1 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB-EBc1 cells | 29435139 | |||
| NB1643 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for NB1643 cells | 29435139 | |||
| A673 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for A673 cells) | 29435139 | |||
| LAN-5 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for LAN-5 cells | 29435139 | |||
| BT-37 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for BT-37 cells | 29435139 | |||
| Rh41 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for Rh41 cells | 29435139 | |||
| Rh30 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for Rh30 cells | 29435139 | |||
| OHS-50 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for OHS-50 cells | 29435139 | |||
| SK-N-SH | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for SK-N-SH cells | 29435139 | |||
| Cliquez pour voir plus de données expérimentales sur la lignée cellulaire | ||||||
| Poids moléculaire | 529.52 | Formule | C28H22F3N7O |
Stockage (À compter de la date de réception) | |
|---|---|---|---|---|---|
| N° CAS | 641571-10-0 | Télécharger le SDF | Stockage des solutions mères |
|
|
| Synonymes | AMN-107 | Smiles | CC1=C(C=C(C=C1)C(=O)NC2=CC(=CC(=C2)C(F)(F)F)N3C=C(N=C3)C)NC4=NC=CC(=N4)C5=CN=CC=C5 | ||
|
In vitro |
DMSO
: 52 mg/mL
(98.2 mM)
Water : Insoluble Ethanol : Insoluble |
|
In vivo |
|||||
Étape 1 : Saisir les informations ci-dessous (Recommandé : Un animal supplémentaire pour tenir compte des pertes pendant lexpérience)
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.)
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.
| Caractéristiques |
A selective inhibitor of native and mutant Bcr-Abl.
|
|---|---|
| Targets/IC50/Ki |
Bcr-Abl
(Murine myeloid progenitor cells) <30 nM
|
| In vitro |
Le Nilotinib inhibe la prolifération, la migration et la formation de filaments d'actine, ainsi que l'expression de l'α-SMA et du collagène dans les HSC activées. Ce composé induit l'apoptose des HSC, ce qui est corrélé à une expression réduite de bcl-2, à une augmentation de l'expression de p53, au clivage de PARP, ainsi qu'à une augmentation de l'expression de PPARγ et de TRAIL-R. Il induit également un arrêt du cycle cellulaire, accompagné d'une expression accrue de p27 et d'une régulation négative de la cycline D1. Fait intéressant, cette substance chimique n'inhibe pas seulement l'activation du PDGFR, mais aussi du TGFRII via Src. Elle inhibe significativement la phosphorylation d'ERK et d'Akt stimulée par le PDGF et le TGFβ. De plus, les formes phosphorylées d'Abl activées par le PDGF et le TGFβ dans les HSC humaines sont inhibées par cet agent. Cet inhibiteur supprime la plupart des mutations de Bcr-Abl résistantes à l'imatinib, à l'exception de T315I. Il inhibe l'activation d'ERK1/2 médiée par le PDGF-DD, l'activation basale et médiée par le PDGF-DD du PDGFRβ et d'Akt, et la prolifération du schwannome. Ce composé est plus puissant que l'imatinib, exerçant son effet inhibiteur maximal à des concentrations inférieures aux taux plasmatiques résiduels à l'état d'équilibre. Il réduit également significativement les niveaux d'expression des gènes du TGF-β1 et du facteur de croissance dérivé des plaquettes (PDGF). Ce traitement inhibe également significativement la prolifération des fibroblastes pulmonaires induite par le PDGF. Il inhibe la prolifération des cellules Ba/F3 exprimant p210- et p190-Bcr-Abl, ou des cellules K562 et Ku-812F avec des valeurs d'IC50 ≤12 nM.
|
| In vivo |
Le Nilotinib réduit le dépôt de collagène et l'expression de l'α-SMA dans la fibrose induite par le CCl4 et le BDL. Ce composé pourrait induire l'apoptose des HSC, ce qui est corrélé à la régulation négative de bcl-2. Il atténue l'étendue des lésions pulmonaires et de la fibrose. Cette thérapie réduit significativement les niveaux d'hydroxyproline aux jours 14 et 21, ce qui s'accompagne d'une diminution des niveaux d'expression du facteur de croissance transformant (TGF)-β1 et du PDGFRβ. Cette substance chimique prolonge la survie des souris injectées avec des lignées cellulaires hématopoïétiques transformées par Bcr-Abl ou des cellules de moelle primaire, et prolonge la survie dans les modèles de souris CML résistantes à l'imatinib.
|
Références |
|
| Méthodes | Biomarqueurs | Images | PMID |
|---|---|---|---|
| Western blot | p-AMPKα / AMPKα / p-AMPKβ1 / AMPKγ2 / p-LKB1 / LKB1 / CaMKIIβ DNMT1 / DNMT3a / DNMT3b pABL1 / p-NF-κB1 / NF-κB / STAT3 / p-STAT3 / IL-1β / IL-6 / COX2 |
|
23677989 |
| Growth inhibition assay | Cell viability |
|
23677989 |
(données du https://clinicaltrials.gov, mis à jour le 2024-05-22)
| Numéro NCT | Recrutement | Conditions | Promoteur/Collaborateurs | Date de début | Phases |
|---|---|---|---|---|---|
| NCT06409936 | Not yet recruiting | CML Chronic Phase|Chronic Myeloid Leukemia Chronic Phase|Chronic Myeloid Leukemia BCR/ABL-Positive|Chronic Myeloid Leukemia |
Gruppo Italiano Malattie EMatologiche dell''Adulto|Fundacion Espanola para la Curacion de la Leucemia Mieloide Cronica |
September 2024 | Phase 2 |
| NCT05185947 | Recruiting | Gynecologic Cancer|Gynecologic Neoplasms|Peritoneal Carcinomatosis|Peritoneal Neoplasms|Ovarian Cancer|Ovarian Neoplasms|Colorectal Cancer|Colorectal Neoplasms|Appendiceal Cancer|Appendiceal Neoplasms |
National Cancer Institute (NCI)|National Institutes of Health Clinical Center (CC) |
October 13 2022 | Phase 2 |
| NCT04326933 | Unknown status | Patients Diagnosed as Chronic Meyloid Leukemia |
Assiut University |
January 1 2020 | -- |
| NCT04002674 | Recruiting | Dementia With Lewy Bodies |
Georgetown University|National Institutes of Health (NIH) |
July 1 2019 | Phase 2 |
Tel: +1-832-582-8158 Ext:3
Si vous avez dautres questions, veuillez laisser un message.
Question 1:
I would like to use it for in vivo studies in mice, can you give me some suggestions about the in vivo formulation?
Réponse :
For in vivo study, we recommend to use 4% DMSO+30% PEG 300+5% Tween 80+ddH2O up to 3mg/ml for it.