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Pictilisib (GDC-0941) inhibiteur de PI3Kα/δ
Réf. CatalogueS1065
Structure chimique
Poids moléculaire: 513.64
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Contrôle Qualité
Lot :
Pureté :
99.97%
99.97
| Cibles apparentées | Akt mTOR GSK-3 ATM/ATR DNA-PK AMPK PDPK1 PTEN PP2A PDK |
|---|---|
| Autre PI3K Inhibiteurs | GDC-0077 (Inavolisib) SAR405 Quercetin (Sophoretin) LY294002 XL147 analogue Tersolisib (STX-478) Buparlisib (BKM120) 740 Y-P (PDGFR 740Y-P) GO-203 TFA Eganelisib (IPI-549) |
Culture cellulaire, traitement et concentration de travail
| Lignées cellulaires | Type dessai | Concentration | Temps dincubation | Formulation | Description de lactivité | PMID |
|---|---|---|---|---|---|---|
| Sf9 | Kinase Assay | 1 h | DMSO | Inhibition of human recombinant PI3K p110delta expressed in Sf9 cells coexpressing p85alpha with IC50 of 0.003 μM | 18754654 | |
| Sf9 | Kinase Assay | 1 h | DMSO | Inhibition of human recombinant PI3K p110beta H1047-R mutant expressed in Sf9 cells coexpressing p85alpha with IC50 of 0.003 μM | 18754654 | |
| Sf9 | Kinase Assay | 1 h | DMSO | Inhibition of human recombinant PI3K p110beta E545-K mutant expressed in Sf9 cells coexpressing p85alpha with IC50 of 0.003 μM | 18754654 | |
| Sf9 | Kinase Assay | 1 h | DMSO | Inhibition of human recombinant PI3K p110beta expressed in Sf9 cells coexpressing p85alpha with IC50 of 0.033 μM | 18754654 | |
| Sf9 | Kinase Assay | 1 h | DMSO | Inhibition of human recombinant PI3K p110alpha expressed in Sf9 cells coexpressing p85alpha | 18754654 | |
| MDA-MB-361 | Function Assay | 2 h | DMSO | Inhibition of Akt Ser473 phosphorylation in human MDA-MB-361 cells with PIK3CA E545-K mutation with IC50 of 0.028 μM | 18754654 | |
| PC3 | Function Assay | 2 h | DMSO | Inhibition of Akt Ser473 phosphorylation in PTEN-null human PC3 cells with IC50 of 0.037 μM | 18754654 | |
| U87MG | Function Assay | 2 h | DMSO | Inhibition of Akt Ser473 phosphorylation in PTEN-null human U87MG cells with IC50 of 0.046 μM | 18754654 | |
| MDA-MB-361 | Growth Inhibition Assay | 96 h | DMSO | Antiproliferative activity against human MDA-MB-361 cells with PIK3CA E545-K mutation with IC50 of 0.72 μM | 18754654 | |
| A2780 | Growth Inhibition Assay | 96 h | DMSO | Antiproliferative activity against human A2780 cells with PIK3CA and PTEN mutation with IC50 of 0.14 μM | 18754654 | |
| PC3 | Growth Inhibition Assay | 96 h | DMSO | IC50=0.28 μM | 18754654 | |
| U87MG | Growth Inhibition Assay | 96 h | DMSO | IC50=0.95 μM | 18754654 | |
| Sf9 | Kinase Assay | 30 min | DMSO | Inhibition of human PI3Kgamma expressed assessed as amount of ATP consumed with IC50 of 0.042 μM | 22548342 | |
| RAW 264.7 | Kinase Assay | 90 min | DMSO | Inhibition of human PI3Kgamma expressed assessed as inhibition of AKT phosphorylation with IC50 of 0.298 μM | 22548342 | |
| Sf9 | Kinase Assay | 1 h | Inhibition of GST-fused human recombinant PI3Kbeta expressed in baculovirus infected SF9 cells with IC50 of 0.017 μM | 23540645 | ||
| Sf9 | Kinase Assay | 1 h | Inhibition of GST-fused human recombinant PI3Kdelta expressed | 23540645 | ||
| Sf9 | Kinase Assay | 1 h | Inhibition of GST-fused human recombinant PI3Kgamma expressed | 23540645 | ||
| Sf9 | Kinase Assay | 1 h | Inhibition of GST-fused human recombinant PI3Kalpha expressed | 23540645 | ||
| SKOV3 | Kinase Assay | 1 μM | 1 h | DMSO | Inhibition of PI3Kalpha assessed as inhibition of Akt Ser473 phosphorylation | 23360348 |
| MCF7 | Growth Inhibition Assay | 1 μM | 96 h | DMSO | GI50=0.0702 μM | 23360348 |
| SKOV3 | Growth Inhibition Assay | 1 μM | 96 h | DMSO | GI50=0.1476 μM | 23360348 |
| PC3 | Growth Inhibition Assay | 72 h | DMSO | IC50=0.28 μM | 21981714 | |
| MCF7.1 | Growth Inhibition Assay | 72 h | DMSO | Antiproliferative activity against human MCF7.1 cells expressing HER2 gene with IC50 of 0.28 μM | 21981714 | |
| MCF7-neo/Her2 | Growth Inhibition Assay | 72 h | DMSO | IC50=0.29 μM | 23662903 | |
| MCF7-neo/Her2 | Kinase Assay | Inhibition of PI3Kalpha assessed as reduction of AKT phosphorylation at S473 with IC50 of 0.007 μM | 23662903 | |||
| PC3 | Growth Inhibition Assay | 72 h | DMSO | EC50=0.34 μM | 21985639 | |
| MCF7.1 | Growth Inhibition Assay | 72 h | DMSO | Antiproliferative activity against human MCF7.1 cells expressing PI3Kalpha mutant with EC50 of 0.39 μM | 21985639 | |
| PC3 | Growth Inhibition Assay | 72 h | DMSO | Antiproliferative activity against human PC3 cells deficient in PTEN with IC50 of 0.39 μM | 20050669 | |
| MCF7.1 | Growth Inhibition Assay | 72 h | DMSO | Antiproliferative activity against human MCF7.1 cells expressing PI3Kalpha mutant with IC50 of 0.34 μM | 20050669 | |
| MCF7.1 | Growth Inhibition Assay | 72 h | EC50=0.72 μM | 20346656 | ||
| NCI-H1975 | Cytotoxic Assay | 72 h | IC50=0.27 μM | 23059545 | ||
| H460 | Cytotoxic Assay | 72 h | IC50=0.87 μM | 23059545 | ||
| HT-29 | Cytotoxic Assay | 72 h | IC50=0.66 μM | 23059545 | ||
| HepG2 | Cytotoxic Assay | 72 h | IC50=1 μM | 23059545 | ||
| SGC7901 | Cytotoxic Assay | 72 h | IC50=1.8 μM | 23059545 | ||
| NCI-H226 | Cytotoxic Assay | 72 h | IC50=2.9 μM | 23059545 | ||
| A549 | Cytotoxic Assay | 72 h | IC50=6.9 μM | 23059545 | ||
| U87MG | Cytotoxic Assay | 72 h | IC50=7.77 μM | 23059545 | ||
| HBC4 | Growth Inhibition Assay | logGI50=-6.03 M | 22336246 | |||
| BSY1 | Growth Inhibition Assay | logGI50=-6.90 M | 22336246 | |||
| HBC5 | Growth Inhibition Assay | logGI50=-6.60 M | 22336246 | |||
| MCF7 | Growth Inhibition Assay | logGI50=-7.33 M | 22336246 | |||
| MDA-MB-231 | Growth Inhibition Assay | logGI50=-5.46 M | 22336246 | |||
| U251 | Growth Inhibition Assay | logGI50=-5.50 M | 22336246 | |||
| SF268 | Growth Inhibition Assay | logGI50=-5.39 M | 22336246 | |||
| SF295 | Growth Inhibition Assay | logGI50=-6.37 M | 22336246 | |||
| SF539 | Growth Inhibition Assay | logGI50=-6.50 M | 22336246 | |||
| SNB75 | Growth Inhibition Assay | logGI50=-7.10 M | 22336246 | |||
| SNB78 | Growth Inhibition Assay | logGI50=-6.52 M | 22336246 | |||
| HCC2998 | Growth Inhibition Assay | logGI50=-6.29 M | 22336246 | |||
| KM12 | Growth Inhibition Assay | logGI50=-5.76 M | 22336246 | |||
| HT-29 | Growth Inhibition Assay | logGI50=-6.30 M | 22336246 | |||
| HCT15 | Growth Inhibition Assay | logGI50=-6.12 M | 22336246 | |||
| HCT116 | Growth Inhibition Assay | logGI50=-5.87 M | 22336246 | |||
| NCI-H23 | Growth Inhibition Assay | logGI50=-5.73 M | 22336246 | |||
| NCI-H226 | Growth Inhibition Assay | logGI50=-6.21 M | 22336246 | |||
| NCI-H522 | Growth Inhibition Assay | logGI50=-6.58 M | 22336246 | |||
| NCI-H483 | Growth Inhibition Assay | logGI50=-6.56 M | 22336246 | |||
| A549 | Growth Inhibition Assay | logGI50=-6.15 M | 22336246 | |||
| DMS273 | Growth Inhibition Assay | logGI50=-6.43 M | 22336246 | |||
| DMS114 | Growth Inhibition Assay | logGI50=-5.92 M | 22336246 | |||
| LOXIMVI | Growth Inhibition Assay | logGI50=-6.29 M | 22336246 | |||
| OVCAR3 | Growth Inhibition Assay | logGI50=-6.71 M | 22336246 | |||
| OVCAR4 | Growth Inhibition Assay | logGI50=-5.76 M | 22336246 | |||
| OVCAR5 | Growth Inhibition Assay | logGI50=-6.26 M | 22336246 | |||
| OVCAR8 | Growth Inhibition Assay | logGI50=-5.73 M | 22336246 | |||
| SKOV3 | Growth Inhibition Assay | logGI50=-6.52 M | 22336246 | |||
| RXF631L | Growth Inhibition Assay | logGI50=-6.88 M | 22336246 | |||
| ACHN | Growth Inhibition Assay | logGI50=-6.07 M | 22336246 | |||
| St-4 | Growth Inhibition Assay | logGI50=-5.56 M | 22336246 | |||
| MKN1 | Growth Inhibition Assay | logGI50=-7.08 M | 22336246 | |||
| MKN7 | Growth Inhibition Assay | logGI50=-6.50 M | 22336246 | |||
| MKN28 | Growth Inhibition Assay | logGI50=-5.52 M | 22336246 | |||
| MKN45 | Growth Inhibition Assay | logGI50=-6.55 M | 22336246 | |||
| MKN74 | Growth Inhibition Assay | logGI50=-6.02 M | 22336246 | |||
| DU145 | Growth Inhibition Assay | logGI50=-5.85 M | 22336246 | |||
| PC3 | Growth Inhibition Assay | logGI50=-6.66 M | 22336246 | |||
| ES5 | Growth Inhibition Assay | IC50=50.21 nM | SANGER | |||
| HH | Growth Inhibition Assay | IC50=111.08 nM | SANGER | |||
| MHH-PREB-1 | Growth Inhibition Assay | IC50=114.3 nM | SANGER | |||
| NCI-H1770 | Growth Inhibition Assay | IC50=123.86 nM | SANGER | |||
| HuO9 | Growth Inhibition Assay | IC50=206.02 nM | SANGER | |||
| HAL-01 | Growth Inhibition Assay | IC50=206.73 nM | SANGER | |||
| NOS-1 | Growth Inhibition Assay | IC50=211.82 nM | SANGER | |||
| HGC-27 | Growth Inhibition Assay | IC50=212.57 nM | SANGER | |||
| NB69 | Growth Inhibition Assay | IC50=245.27 nM | SANGER | |||
| RS4-11 | Growth Inhibition Assay | IC50=261.76 nM | SANGER | |||
| DOK | Growth Inhibition Assay | IC50=301.7 nM | SANGER | |||
| LB2241-RCC | Growth Inhibition Assay | IC50=303.84 nM | SANGER | |||
| NCI-H1623 | Growth Inhibition Assay | IC50=304.08 nM | SANGER | |||
| YH-13 | Growth Inhibition Assay | IC50=304.32 nM | SANGER | |||
| BPH-1 | Growth Inhibition Assay | IC50=314 nM | SANGER | |||
| AN3-CA | Growth Inhibition Assay | IC50=340.37 nM | SANGER | |||
| ES7 | Growth Inhibition Assay | IC50=341.99 nM | SANGER | |||
| MDA-MB-175-VII | Growth Inhibition Assay | IC50=352.92 nM | SANGER | |||
| GAMG | Growth Inhibition Assay | IC50=370.85 nM | SANGER | |||
| CHL-1 | Growth Inhibition Assay | IC50=378.65 nM | SANGER | |||
| NB7 | Growth Inhibition Assay | IC50=389.83 nM | SANGER | |||
| MFE-280 | Growth Inhibition Assay | IC50=418.2 nM | SANGER | |||
| HL-60 | Growth Inhibition Assay | IC50=425.75 nM | SANGER | |||
| GCIY | Growth Inhibition Assay | IC50=433.8 nM | SANGER | |||
| MDA-MB-361 | Growth Inhibition Assay | IC50=439.13 nM | SANGER | |||
| LXF-289 | Growth Inhibition Assay | IC50=448.27 nM | SANGER | |||
| NBsusSR | Growth Inhibition Assay | IC50=488.85 nM | SANGER | |||
| KU-19-19 | Growth Inhibition Assay | IC50=516.07 nM | SANGER | |||
| A204 | Growth Inhibition Assay | IC50=522.33 nM | SANGER | |||
| LB1047-RCC | Growth Inhibition Assay | IC50=522.93 nM | SANGER | |||
| COLO-684 | Growth Inhibition Assay | IC50=523.11 nM | SANGER | |||
| PA-1 | Growth Inhibition Assay | IC50=532.41 nM | SANGER | |||
| MG-63 | Growth Inhibition Assay | IC50=541.11 nM | SANGER | |||
| BHT-101 | Growth Inhibition Assay | IC50=544.94 nM | SANGER | |||
| NKM-1 | Growth Inhibition Assay | IC50=593.09 nM | SANGER | |||
| T47D | Growth Inhibition Assay | IC50=597.56 nM | SANGER | |||
| MOLT-4 | Growth Inhibition Assay | IC50=623.62 nM | SANGER | |||
| IGROV-1 | Growth Inhibition Assay | IC50=634.31 nM | SANGER | |||
| ES4 | Growth Inhibition Assay | IC50=639.54 nM | SANGER | |||
| HuO-3N1 | Growth Inhibition Assay | IC50=642.38 nM | SANGER | |||
| NEC8 | Growth Inhibition Assay | IC50=653.57 nM | SANGER | |||
| HO-1-N-1 | Growth Inhibition Assay | IC50=659.17 nM | SANGER | |||
| EPCL-272H | Growth Inhibition Assay | IC50=687.21 nM | SANGER | |||
| D-263MG | Growth Inhibition Assay | IC50=718.1 nM | SANGER | |||
| MV-4-11 | Growth Inhibition Assay | IC50=724.31 nM | SANGER | |||
| SK-NEP-1 | Growth Inhibition Assay | IC50=725.94 nM | SANGER | |||
| SW872 | Growth Inhibition Assay | IC50=727.89 nM | SANGER | |||
| P30-OHK | Growth Inhibition Assay | IC50=730.71 nM | SANGER | |||
| OMC-1 | Growth Inhibition Assay | IC50=751.09 nM | SANGER | |||
| LoVo | Growth Inhibition Assay | IC50=777.9 nM | SANGER | |||
| LNCaP-Clone-FGC | Growth Inhibition Assay | IC50=796.34 nM | SANGER | |||
| L-363 | Growth Inhibition Assay | IC50=798.42 nM | SANGER | |||
| ES8 | Growth Inhibition Assay | IC50=810.52 nM | SANGER | |||
| 697 | Growth Inhibition Assay | IC50=831.55 nM | SANGER | |||
| HSC-3 | Growth Inhibition Assay | IC50=839.54 nM | SANGER | |||
| H4 | Growth Inhibition Assay | IC50=850.85 nM | SANGER | |||
| QIMR-WIL | Growth Inhibition Assay | IC50=865.2 nM | SANGER | |||
| OAW-42 | Growth Inhibition Assay | IC50=872.19 nM | SANGER | |||
| MCF7 | Growth Inhibition Assay | IC50=898.59 nM | SANGER | |||
| SCC-25 | Growth Inhibition Assay | IC50=914.19 nM | SANGER | |||
| NCI-H1563 | Growth Inhibition Assay | IC50=915.99 nM | SANGER | |||
| OVCAR-5 | Growth Inhibition Assay | IC50=940.17 nM | SANGER | |||
| HDLM-2 | Growth Inhibition Assay | IC50=949.2 nM | SANGER | |||
| NB5 | Growth Inhibition Assay | IC50=956.6 nM | SANGER | |||
| NCI-H292 | Growth Inhibition Assay | IC50=974.32 nM | SANGER | |||
| A101D | Growth Inhibition Assay | IC50=990.19 nM | SANGER | |||
| NCI-H1648 | Growth Inhibition Assay | IC50=998.51 nM | SANGER | |||
| EKVX | Growth Inhibition Assay | IC50=1.0129 μM | SANGER | |||
| SW1710 | Growth Inhibition Assay | IC50=1.04233 μM | SANGER | |||
| WM-115 | Growth Inhibition Assay | IC50=1.06656 μM | SANGER | |||
| CAL-54 | Growth Inhibition Assay | IC50=1.07081 μM | SANGER | |||
| TGBC24TKB | Growth Inhibition Assay | IC50=1.08045 μM | SANGER | |||
| NCI-H520 | Growth Inhibition Assay | IC50=1.08967 μM | SANGER | |||
| D-423MG | Growth Inhibition Assay | IC50=1.09962 μM | SANGER | |||
| BFTC-905 | Growth Inhibition Assay | IC50=1.13449 μM | SANGER | |||
| HT | Growth Inhibition Assay | IC50=1.13478 μM | SANGER | |||
| CTB-1 | Growth Inhibition Assay | IC50=1.14293 μM | SANGER | |||
| Hs-578-T | Growth Inhibition Assay | IC50=1.19565 μM | SANGER | |||
| HuH-7 | Growth Inhibition Assay | IC50=1.20949 μM | SANGER | |||
| LB996-RCC | Growth Inhibition Assay | IC50=1.22177 μM | SANGER | |||
| KYSE-270 | Growth Inhibition Assay | IC50=1.29734 μM | SANGER | |||
| A4-Fuk | Growth Inhibition Assay | IC50=1.29993 μM | SANGER | |||
| A498 | Growth Inhibition Assay | IC50=1.30474 μM | SANGER | |||
| SK-MEL-1 | Growth Inhibition Assay | IC50=1.30679 μM | SANGER | |||
| AU565 | Growth Inhibition Assay | IC50=1.31863 μM | SANGER | |||
| Saos-2 | Growth Inhibition Assay | IC50=1.33205 μM | SANGER | |||
| A549 | Growth Inhibition Assay | IC50=1.3997 μM | SANGER | |||
| BFTC-909 | Growth Inhibition Assay | IC50=1.43305 μM | SANGER | |||
| MDA-MB-415 | Growth Inhibition Assay | IC50=1.48692 μM | SANGER | |||
| 639-V | Growth Inhibition Assay | IC50=1.50245 μM | SANGER | |||
| A704 | Growth Inhibition Assay | IC50=1.50785 μM | SANGER | |||
| PANC-03-27 | Growth Inhibition Assay | IC50=1.51408 μM | SANGER | |||
| SK-MEL-28 | Growth Inhibition Assay | IC50=1.56085 μM | SANGER | |||
| Ramos-2G6-4C10 | Growth Inhibition Assay | IC50=1.60746 μM | SANGER | |||
| HuP-T4 | Growth Inhibition Assay | IC50=1.60778 μM | SANGER | |||
| VA-ES-BJ | Growth Inhibition Assay | IC50=1.6127 μM | SANGER | |||
| EFM-19 | Growth Inhibition Assay | IC50=1.6181 μM | SANGER | |||
| G-401 | Growth Inhibition Assay | IC50=1.62164 μM | SANGER | |||
| D-566MG | Growth Inhibition Assay | IC50=1.6253 μM | SANGER | |||
| JVM-3 | Growth Inhibition Assay | IC50=1.64875 μM | SANGER | |||
| TK10 | Growth Inhibition Assay | IC50=1.67083 μM | SANGER | |||
| BT-20 | Growth Inhibition Assay | IC50=1.68902 μM | SANGER | |||
| EGI-1 | Growth Inhibition Assay | IC50=1.84701 μM | SANGER | |||
| EW-16 | Growth Inhibition Assay | IC50=1.85182 μM | SANGER | |||
| NCI-H2228 | Growth Inhibition Assay | IC50=1.85203 μM | SANGER | |||
| BB49-HNC | Growth Inhibition Assay | IC50=1.88692 μM | SANGER | |||
| G-402 | Growth Inhibition Assay | IC50=1.89797 μM | SANGER | |||
| NCI-H526 | Growth Inhibition Assay | IC50=1.9139 μM | SANGER | |||
| ME-180 | Growth Inhibition Assay | IC50=1.93477 μM | SANGER | |||
| PFSK-1 | Growth Inhibition Assay | IC50=1.94458 μM | SANGER | |||
| TYK-nu | Growth Inhibition Assay | IC50=1.95823 μM | SANGER | |||
| HOS | Growth Inhibition Assay | IC50=1.97948 μM | SANGER | |||
| T98G | Growth Inhibition Assay | IC50=1.99006 μM | SANGER | |||
| SK-MES-1 | Growth Inhibition Assay | IC50=2.01332 μM | SANGER | |||
| SNB75 | Growth Inhibition Assay | IC50=2.01541 μM | SANGER | |||
| LAMA-84 | Growth Inhibition Assay | IC50=2.02689 μM | SANGER | |||
| CAL-39 | Growth Inhibition Assay | IC50=2.0328 μM | SANGER | |||
| LOXIMVI | Growth Inhibition Assay | IC50=2.04084 μM | SANGER | |||
| NH-12 | Growth Inhibition Assay | IC50=2.05424 μM | SANGER | |||
| NCI-H1048 | Growth Inhibition Assay | IC50=2.1052 μM | SANGER | |||
| KS-1 | Growth Inhibition Assay | IC50=2.11001 μM | SANGER | |||
| NCI-N87 | Growth Inhibition Assay | IC50=2.13384 μM | SANGER | |||
| CHP-212 | Growth Inhibition Assay | IC50=2.18442 μM | SANGER | |||
| HCC1419 | Growth Inhibition Assay | IC50=2.21115 μM | SANGER | |||
| ES1 | Growth Inhibition Assay | IC50=2.21326 μM | SANGER | |||
| NCI-H2030 | Growth Inhibition Assay | IC50=2.24123 μM | SANGER | |||
| EW-22 | Growth Inhibition Assay | IC50=2.25067 μM | SANGER | |||
| A431 | Growth Inhibition Assay | IC50=2.27354 μM | SANGER | |||
| SF126 | Growth Inhibition Assay | IC50=2.30625 μM | SANGER | |||
| SF295 | Growth Inhibition Assay | IC50=2.31524 μM | SANGER | |||
| D-502MG | Growth Inhibition Assay | IC50=2.32461 μM | SANGER | |||
| HCC2157 | Growth Inhibition Assay | IC50=2.32927 μM | SANGER | |||
| D-283MED | Growth Inhibition Assay | IC50=2.35926 μM | SANGER | |||
| SNU-423 | Growth Inhibition Assay | IC50=2.40171 μM | SANGER | |||
| SK-LU-1 | Growth Inhibition Assay | IC50=2.44586 μM | SANGER | |||
| 22RV1 | Growth Inhibition Assay | IC50=2.45617 μM | SANGER | |||
| SW1088 | Growth Inhibition Assay | IC50=2.49213 μM | SANGER | |||
| HT-3 | Growth Inhibition Assay | IC50=2.49259 μM | SANGER | |||
| NCI-H1666 | Growth Inhibition Assay | IC50=2.51104 μM | SANGER | |||
| EM-2 | Growth Inhibition Assay | IC50=2.51169 μM | SANGER | |||
| SNU-449 | Growth Inhibition Assay | IC50=2.57014 μM | SANGER | |||
| 786-0 | Growth Inhibition Assay | IC50=2.59238 μM | SANGER | |||
| SKG-IIIa | Growth Inhibition Assay | IC50=2.65939 μM | SANGER | |||
| MEL-HO | Growth Inhibition Assay | IC50=2.67634 μM | SANGER | |||
| LCLC-97TM1 | Growth Inhibition Assay | IC50=2.69267 μM | SANGER | |||
| MKN7 | Growth Inhibition Assay | IC50=2.70754 μM | SANGER | |||
| 5637 | Growth Inhibition Assay | IC50=2.71035 μM | SANGER | |||
| HOP-92 | Growth Inhibition Assay | IC50=2.74717 μM | SANGER | |||
| MDA-MB-157 | Growth Inhibition Assay | IC50=2.82023 μM | SANGER | |||
| NB12 | Growth Inhibition Assay | IC50=2.84914 μM | SANGER | |||
| DMS-273 | Growth Inhibition Assay | IC50=2.8647 μM | SANGER | |||
| HCC70 | Growth Inhibition Assay | IC50=2.86589 μM | SANGER | |||
| YKG-1 | Growth Inhibition Assay | IC50=3.03787 μM | SANGER | |||
| NCI-H28 | Growth Inhibition Assay | IC50=3.05291 μM | SANGER | |||
| HN | Growth Inhibition Assay | IC50=3.06636 μM | SANGER | |||
| HT-1080 | Growth Inhibition Assay | IC50=3.08606 μM | SANGER | |||
| HPAF-II | Growth Inhibition Assay | IC50=3.10068 μM | SANGER | |||
| U-2-OS | Growth Inhibition Assay | IC50=3.13782 μM | SANGER | |||
| SNU-387 | Growth Inhibition Assay | IC50=3.16364 μM | SANGER | |||
| Becker | Growth Inhibition Assay | IC50=3.16808 μM | SANGER | |||
| BHY | Growth Inhibition Assay | IC50=3.25571 μM | SANGER | |||
| HTC-C3 | Growth Inhibition Assay | IC50=3.29352 μM | SANGER | |||
| M14 | Growth Inhibition Assay | IC50=3.30663 μM | SANGER | |||
| COR-L23 | Growth Inhibition Assay | IC50=3.37279 μM | SANGER | |||
| C32 | Growth Inhibition Assay | IC50=3.41508 μM | SANGER | |||
| Mewo | Growth Inhibition Assay | IC50=3.42182 μM | SANGER | |||
| TE-8 | Growth Inhibition Assay | IC50=3.48259 μM | SANGER | |||
| RPMI-2650 | Growth Inhibition Assay | IC50=3.60637 μM | SANGER | |||
| AGS | Growth Inhibition Assay | IC50=3.62464 μM | SANGER | |||
| MZ2-MEL | Growth Inhibition Assay | IC50=3.66138 μM | SANGER | |||
| Calu-3 | Growth Inhibition Assay | IC50=3.71287 μM | SANGER | |||
| SJSA-1 | Growth Inhibition Assay | IC50=3.71315 μM | SANGER | |||
| SW962 | Growth Inhibition Assay | IC50=3.72636 μM | SANGER | |||
| PC-14 | Growth Inhibition Assay | IC50=3.73222 μM | SANGER | |||
| SW1573 | Growth Inhibition Assay | IC50=3.75348 μM | SANGER | |||
| 769-P | Growth Inhibition Assay | IC50=3.82743 μM | SANGER | |||
| KNS-62 | Growth Inhibition Assay | IC50=3.92338 μM | SANGER | |||
| NCI-H747 | Growth Inhibition Assay | IC50=4.05638 μM | SANGER | |||
| LN-405 | Growth Inhibition Assay | IC50=4.15728 μM | SANGER | |||
| OVCAR-8 | Growth Inhibition Assay | IC50=4.22543 μM | SANGER | |||
| DMS-114 | Growth Inhibition Assay | IC50=4.23891 μM | SANGER | |||
| NCI-H2126 | Growth Inhibition Assay | IC50=4.24558 μM | SANGER | |||
| TCCSUP | Growth Inhibition Assay | IC50=4.24788 μM | SANGER | |||
| SK-N-FI | Growth Inhibition Assay | IC50=4.25332 μM | SANGER | |||
| HCE-4 | Growth Inhibition Assay | IC50=4.27197 μM | SANGER | |||
| DK-MG | Growth Inhibition Assay | IC50=4.3039 μM | SANGER | |||
| RO82-W-1 | Growth Inhibition Assay | IC50=4.32584 μM | SANGER | |||
| A2780 | Growth Inhibition Assay | IC50=4.36682 μM | SANGER | |||
| ETK-1 | Growth Inhibition Assay | IC50=4.37052 μM | SANGER | |||
| FADU | Growth Inhibition Assay | IC50=4.37467 μM | SANGER | |||
| CAL-12T | Growth Inhibition Assay | IC50=4.41413 μM | SANGER | |||
| 647-V | Growth Inhibition Assay | IC50=4.44022 μM | SANGER | |||
| TGBC1TKB | Growth Inhibition Assay | IC50=4.45113 μM | SANGER | |||
| LU-99A | Growth Inhibition Assay | IC50=4.4606 μM | SANGER | |||
| CAL-33 | Growth Inhibition Assay | IC50=4.52456 μM | SANGER | |||
| LU-134-A | Growth Inhibition Assay | IC50=4.52745 μM | SANGER | |||
| NCI-H1355 | Growth Inhibition Assay | IC50=4.55146 μM | SANGER | |||
| RPMI-7951 | Growth Inhibition Assay | IC50=4.57002 μM | SANGER | |||
| TE-1 | Growth Inhibition Assay | IC50=4.66143 μM | SANGER | |||
| OE33 | Growth Inhibition Assay | IC50=4.70511 μM | SANGER | |||
| CAL-51 | Growth Inhibition Assay | IC50=4.71082 μM | SANGER | |||
| SW1783 | Growth Inhibition Assay | IC50=4.75308 μM | SANGER | |||
| BT-474 | Growth Inhibition Assay | IC50=4.76384 μM | SANGER | |||
| KYSE-520 | Growth Inhibition Assay | IC50=4.87392 μM | SANGER | |||
| 8-MG-BA | Growth Inhibition Assay | IC50=4.88557 μM | SANGER | |||
| IA-LM | Growth Inhibition Assay | IC50=4.99435 μM | SANGER | |||
| SW954 | Growth Inhibition Assay | IC50=4.99443 μM | SANGER | |||
| RPMI-8226 | Growth Inhibition Assay | IC50=5.05461 μM | SANGER | |||
| MKN1 | Growth Inhibition Assay | IC50=5.07927 μM | SANGER | |||
| A375 | Growth Inhibition Assay | IC50=5.09256 μM | SANGER | |||
| 8305C | Growth Inhibition Assay | IC50=5.09887 μM | SANGER | |||
| CAL-62 | Growth Inhibition Assay | IC50=5.18259 μM | SANGER | |||
| NB10 | Growth Inhibition Assay | IC50=5.22744 μM | SANGER | |||
| OC-314 | Growth Inhibition Assay | IC50=5.37444 μM | SANGER | |||
| PSN1 | Growth Inhibition Assay | IC50=5.38286 μM | SANGER | |||
| GR-ST | Growth Inhibition Assay | IC50=5.38322 μM | SANGER | |||
| P12-ICHIKAWA | Growth Inhibition Assay | IC50=5.401 μM | SANGER | |||
| NCI-H1092 | Growth Inhibition Assay | IC50=5.41148 μM | SANGER | |||
| SCC-4 | Growth Inhibition Assay | IC50=5.41355 μM | SANGER | |||
| TE-6 | Growth Inhibition Assay | IC50=5.41816 μM | SANGER | |||
| DOHH-2 | Growth Inhibition Assay | IC50=5.42248 μM | SANGER | |||
| SW684 | Growth Inhibition Assay | IC50=5.66385 μM | SANGER | |||
| CP50-MEL-B | Growth Inhibition Assay | IC50=5.68684 μM | SANGER | |||
| UM-UC-3 | Growth Inhibition Assay | IC50=5.72231 μM | SANGER | |||
| LC-2-ad | Growth Inhibition Assay | IC50=5.78251 μM | SANGER | |||
| PC-3 | Growth Inhibition Assay | IC50=5.91615 μM | SANGER | |||
| CAN | Growth Inhibition Assay | IC50=5.9282 μM | SANGER | |||
| ESS-1 | Growth Inhibition Assay | IC50=5.97869 μM | SANGER | |||
| ATN-1 | Growth Inhibition Assay | IC50=6.05568 μM | SANGER | |||
| BxPC-3 | Growth Inhibition Assay | IC50=6.08219 μM | SANGER | |||
| KYSE-150 | Growth Inhibition Assay | IC50=6.12476 μM | SANGER | |||
| RPMI-8866 | Growth Inhibition Assay | IC50=6.19163 μM | SANGER | |||
| SW780 | Growth Inhibition Assay | IC50=6.2042 μM | SANGER | |||
| A388 | Growth Inhibition Assay | IC50=6.23115 μM | SANGER | |||
| NCI-H1437 | Growth Inhibition Assay | IC50=6.24073 μM | SANGER | |||
| NCI-H1755 | Growth Inhibition Assay | IC50=6.36612 μM | SANGER | |||
| LS-123 | Growth Inhibition Assay | IC50=6.40521 μM | SANGER | |||
| CaR-1 | Growth Inhibition Assay | IC50=6.46373 μM | SANGER | |||
| RT-112 | Growth Inhibition Assay | IC50=6.60338 μM | SANGER | |||
| CGT | Growth Inhibition Assay | IC50=6.73681 μM | SANGER | |||
| SW626 | Growth Inhibition Assay | IC50=6.73946 μM | SANGER | |||
| AsPC-1 | Growth Inhibition Assay | IC50=6.74507 μM | SANGER | |||
| SBC-5 | Growth Inhibition Assay | IC50=6.97297 μM | SANGER | |||
| SF539 | Growth Inhibition Assay | IC50=6.99333 μM | SANGER | |||
| TI-73 | Growth Inhibition Assay | IC50=7.06285 μM | SANGER | |||
| MHH-ES-1 | Growth Inhibition Assay | IC50=7.07762 μM | SANGER | |||
| KYSE-510 | Growth Inhibition Assay | IC50=7.08432 μM | SANGER | |||
| EW-1 | Growth Inhibition Assay | IC50=7.36996 μM | SANGER | |||
| SK-OV-3 | Growth Inhibition Assay | IC50=7.39432 μM | SANGER | |||
| MC-IXC | Growth Inhibition Assay | IC50=7.41972 μM | SANGER | |||
| HSC-2 | Growth Inhibition Assay | IC50=7.42705 μM | SANGER | |||
| NCI-H2342 | Growth Inhibition Assay | IC50=7.5149 μM | SANGER | |||
| NCI-H1792 | Growth Inhibition Assay | IC50=7.51711 μM | SANGER | |||
| HT-1376 | Growth Inhibition Assay | IC50=7.87778 μM | SANGER | |||
| EW-13 | Growth Inhibition Assay | IC50=7.89977 μM | SANGER | |||
| no-11 | Growth Inhibition Assay | IC50=7.90174 μM | SANGER | |||
| Daoy | Growth Inhibition Assay | IC50=7.94321 μM | SANGER | |||
| COLO-800 | Growth Inhibition Assay | IC50=8.04162 μM | SANGER | |||
| GB-1 | Growth Inhibition Assay | IC50=8.06565 μM | SANGER | |||
| SJRH30 | Growth Inhibition Assay | IC50=8.15878 μM | SANGER | |||
| NCI-H2291 | Growth Inhibition Assay | IC50=8.29187 μM | SANGER | |||
| J82 | Growth Inhibition Assay | IC50=8.29491 μM | SANGER | |||
| NCI-H596 | Growth Inhibition Assay | IC50=8.31453 μM | SANGER | |||
| RERF-LC-MS | Growth Inhibition Assay | IC50=8.34856 μM | SANGER | |||
| RH-18 | Growth Inhibition Assay | IC50=8.35046 μM | SANGER | |||
| SW48 | Growth Inhibition Assay | IC50=8.59453 μM | SANGER | |||
| RD | Growth Inhibition Assay | IC50=8.59391 μM | SANGER | |||
| MS-1 | Growth Inhibition Assay | IC50=8.61387 μM | SANGER | |||
| ES6 | Growth Inhibition Assay | IC50=8.73119 μM | SANGER | |||
| TE-12 | Growth Inhibition Assay | IC50=8.77505 μM | SANGER | |||
| DBTRG-05MG | Growth Inhibition Assay | IC50=8.91217 μM | SANGER | |||
| KINGS-1 | Growth Inhibition Assay | IC50=8.92938 μM | SANGER | |||
| HLE | Growth Inhibition Assay | IC50=8.93785 μM | SANGER | |||
| MHH-NB-11 | Growth Inhibition Assay | IC50=9.01839 μM | SANGER | |||
| U-87-MG | Growth Inhibition Assay | IC50=9.24321 μM | SANGER | |||
| MN-60 | Growth Inhibition Assay | IC50=9.24542 μM | SANGER | |||
| SAS | Growth Inhibition Assay | IC50=9.25581 μM | SANGER | |||
| NCI-H446 | Growth Inhibition Assay | IC50=9.361 μM | SANGER | |||
| C-33-A | Growth Inhibition Assay | IC50=9.43988 μM | SANGER | |||
| RXF393 | Growth Inhibition Assay | IC50=9.47002 μM | SANGER | |||
| CGTH-W-1 | Growth Inhibition Assay | IC50=9.49384 μM | SANGER | |||
| RCM-1 | Growth Inhibition Assay | IC50=9.63801 μM | SANGER | |||
| SN12C | Growth Inhibition Assay | IC50=9.65338 μM | SANGER | |||
| KLE | Growth Inhibition Assay | IC50=9.70009 μM | SANGER | |||
| EFO-21 | Growth Inhibition Assay | IC50=9.77382 μM | SANGER | |||
| KYSE-70 | Growth Inhibition Assay | IC50=9.88011 μM | SANGER | |||
| D-247MG | Growth Inhibition Assay | IC50=10.0568 μM | SANGER | |||
| MPP-89 | Growth Inhibition Assay | IC50=10.0946 μM | SANGER | |||
| RVH-421 | Growth Inhibition Assay | IC50=10.1505 μM | SANGER | |||
| NCI-H460 | Growth Inhibition Assay | IC50=10.2806 μM | SANGER | |||
| NOMO-1 | Growth Inhibition Assay | IC50=10.3532 μM | SANGER | |||
| DEL | Growth Inhibition Assay | IC50=10.3794 μM | SANGER | |||
| HT55 | Growth Inhibition Assay | IC50=10.6205 μM | SANGER | |||
| MC116 | Growth Inhibition Assay | IC50=10.6655 μM | SANGER | |||
| BB30-HNC | Growth Inhibition Assay | IC50=10.669 μM | SANGER | |||
| DJM-1 | Growth Inhibition Assay | IC50=10.6949 μM | SANGER | |||
| ZR-75-30 | Growth Inhibition Assay | IC50=10.9441 μM | SANGER | |||
| U-118-MG | Growth Inhibition Assay | IC50=10.9896 μM | SANGER | |||
| MSTO-211H | Growth Inhibition Assay | IC50=11.0716 μM | SANGER | |||
| SW837 | Growth Inhibition Assay | IC50=11.0949 μM | SANGER | |||
| HuCCT1 | Growth Inhibition Assay | IC50=11.1281 μM | SANGER | |||
| RCC10RGB | Growth Inhibition Assay | IC50=11.135 μM | SANGER | |||
| NMC-G1 | Growth Inhibition Assay | IC50=11.1493 μM | SANGER | |||
| NCI-H650 | Growth Inhibition Assay | IC50=11.3794 μM | SANGER | |||
| HEC-1 | Growth Inhibition Assay | IC50=11.4328 μM | SANGER | |||
| DU-4475 | Growth Inhibition Assay | IC50=11.7393 μM | SANGER | |||
| DSH1 | Growth Inhibition Assay | IC50=11.7606 μM | SANGER | |||
| HCC1569 | Growth Inhibition Assay | IC50=11.7678 μM | SANGER | |||
| HCC1187 | Growth Inhibition Assay | IC50=11.8588 μM | SANGER | |||
| EW-11 | Growth Inhibition Assay | IC50=11.9474 μM | SANGER | |||
| LB2518-MEL | Growth Inhibition Assay | IC50=12.059 μM | SANGER | |||
| KALS-1 | Growth Inhibition Assay | IC50=12.8553 μM | SANGER | |||
| 8505C | Growth Inhibition Assay | IC50=12.885 μM | SANGER | |||
| SK-N-DZ | Growth Inhibition Assay | IC50=13.0453 μM | SANGER | |||
| CHP-134 | Growth Inhibition Assay | IC50=13.1158 μM | SANGER | |||
| HCE-T | Growth Inhibition Assay | IC50=13.2364 μM | SANGER | |||
| LB-831-BLC | Growth Inhibition Assay | IC50=13.6246 μM | SANGER | |||
| OVCAR-4 | Growth Inhibition Assay | IC50=13.6524 μM | SANGER | |||
| SW756 | Growth Inhibition Assay | IC50=13.7246 μM | SANGER | |||
| OCUB-M | Growth Inhibition Assay | IC50=13.8156 μM | SANGER | |||
| SW982 | Growth Inhibition Assay | IC50=13.8276 μM | SANGER | |||
| DB | Growth Inhibition Assay | IC50=13.8384 μM | SANGER | |||
| H-EMC-SS | Growth Inhibition Assay | IC50=13.9139 μM | SANGER | |||
| VMRC-RCZ | Growth Inhibition Assay | IC50=14.0015 μM | SANGER | |||
| CAKI-1 | Growth Inhibition Assay | IC50=14.0132 μM | SANGER | |||
| GI-1 | Growth Inhibition Assay | IC50=14.0658 μM | SANGER | |||
| Ca9-22 | Growth Inhibition Assay | IC50=14.6054 μM | SANGER | |||
| TE-5 | Growth Inhibition Assay | IC50=14.7208 μM | SANGER | |||
| EFO-27 | Growth Inhibition Assay | IC50=14.7622 μM | SANGER | |||
| CAL-72 | Growth Inhibition Assay | IC50=14.7783 μM | SANGER | |||
| GP5d | Growth Inhibition Assay | IC50=15.0474 μM | SANGER | |||
| CAS-1 | Growth Inhibition Assay | IC50=15.066 μM | SANGER | |||
| A2058 | Growth Inhibition Assay | IC50=15.5638 μM | SANGER | |||
| PANC-08-13 | Growth Inhibition Assay | IC50=15.6859 μM | SANGER | |||
| Detroit562 | Growth Inhibition Assay | IC50=15.9139 μM | SANGER | |||
| PANC-10-05 | Growth Inhibition Assay | IC50=16.0821 μM | SANGER | |||
| KOSC-2 | Growth Inhibition Assay | IC50=16.1125 μM | SANGER | |||
| GT3TKB | Growth Inhibition Assay | IC50=16.1981 μM | SANGER | |||
| KM-H2 | Growth Inhibition Assay | IC50=16.3646 μM | SANGER | |||
| LB771-HNC | Growth Inhibition Assay | IC50=16.4422 μM | SANGER | |||
| SF268 | Growth Inhibition Assay | IC50=16.452 μM | SANGER | |||
| OE19 | Growth Inhibition Assay | IC50=16.524 μM | SANGER | |||
| MLMA | Growth Inhibition Assay | IC50=16.5571 μM | SANGER | |||
| MDA-MB-231 | Growth Inhibition Assay | IC50=16.7136 μM | SANGER | |||
| TGW | Growth Inhibition Assay | IC50=16.8102 μM | SANGER | |||
| MDA-MB-453 | Growth Inhibition Assay | IC50=17.0003 μM | SANGER | |||
| SNU-C2B | Growth Inhibition Assay | IC50=17.0237 μM | SANGER | |||
| A427 | Growth Inhibition Assay | IC50=17.2334 μM | SANGER | |||
| SK-MEL-2 | Growth Inhibition Assay | IC50=17.3213 μM | SANGER | |||
| KURAMOCHI | Growth Inhibition Assay | IC50=17.3897 μM | SANGER | |||
| IST-MEL1 | Growth Inhibition Assay | IC50=17.9182 μM | SANGER | |||
| NCI-H1793 | Growth Inhibition Assay | IC50=18.1581 μM | SANGER | |||
| HCC1395 | Growth Inhibition Assay | IC50=18.5611 μM | SANGER | |||
| NUGC-3 | Growth Inhibition Assay | IC50=18.6584 μM | SANGER | |||
| BB65-RCC | Growth Inhibition Assay | IC50=18.669 μM | SANGER | |||
| RMG-I | Growth Inhibition Assay | IC50=18.7382 μM | SANGER | |||
| LS-513 | Growth Inhibition Assay | IC50=18.9228 μM | SANGER | |||
| MFM-223 | Growth Inhibition Assay | IC50=19.0716 μM | SANGER | |||
| NCI-H727 | Growth Inhibition Assay | IC50=19.3295 μM | SANGER | |||
| KP-4 | Growth Inhibition Assay | IC50=19.8531 μM | SANGER | |||
| NB13 | Growth Inhibition Assay | IC50=19.8839 μM | SANGER | |||
| UACC-893 | Growth Inhibition Assay | IC50=19.9757 μM | SANGER | |||
| HT-1197 | Growth Inhibition Assay | IC50=20.2958 μM | SANGER | |||
| NCI-H2029 | Growth Inhibition Assay | IC50=20.3266 μM | SANGER | |||
| GI-ME-N | Growth Inhibition Assay | IC50=20.3373 μM | SANGER | |||
| OVCAR-3 | Growth Inhibition Assay | IC50=20.5822 μM | SANGER | |||
| HD-MY-Z | Growth Inhibition Assay | IC50=21.3696 μM | SANGER | |||
| NTERA-S-cl-D1 | Growth Inhibition Assay | IC50=21.6722 μM | SANGER | |||
| SCH | Growth Inhibition Assay | IC50=22.496 μM | SANGER | |||
| KARPAS-299 | Growth Inhibition Assay | IC50=23.3887 μM | SANGER | |||
| NCI-H1650 | Growth Inhibition Assay | IC50=23.9241 μM | SANGER | |||
| ACHN | Growth Inhibition Assay | IC50=24.4656 μM | SANGER | |||
| M059J | Growth Inhibition Assay | IC50=24.5634 μM | SANGER | |||
| AM-38 | Growth Inhibition Assay | IC50=25.481 μM | SANGER | |||
| KG-1 | Growth Inhibition Assay | IC50=25.5494 μM | SANGER | |||
| COLO-824 | Growth Inhibition Assay | IC50=25.5599 μM | SANGER | |||
| NCI-H1155 | Growth Inhibition Assay | IC50=25.5847 μM | SANGER | |||
| NCI-H441 | Growth Inhibition Assay | IC50=25.7465 μM | SANGER | |||
| J-RT3-T3-5 | Growth Inhibition Assay | IC50=26.3027 μM | SANGER | |||
| JEG-3 | Growth Inhibition Assay | IC50=26.6805 μM | SANGER | |||
| RKO | Growth Inhibition Assay | IC50=26.7632 μM | SANGER | |||
| CAL-85-1 | Growth Inhibition Assay | IC50=27.2118 μM | SANGER | |||
| CAL-120 | Growth Inhibition Assay | IC50=27.6914 μM | SANGER | |||
| NCI-H2452 | Growth Inhibition Assay | IC50=27.7716 μM | SANGER | |||
| NCI-H1395 | Growth Inhibition Assay | IC50=27.7833 μM | SANGER | |||
| KYSE-450 | Growth Inhibition Assay | IC50=27.9862 μM | SANGER | |||
| S-117 | Growth Inhibition Assay | IC50=29.3857 μM | SANGER | |||
| SW13 | Growth Inhibition Assay | IC50=29.8519 μM | SANGER | |||
| ES3 | Growth Inhibition Assay | IC50=30.3733 μM | SANGER | |||
| HCT-116 | Growth Inhibition Assay | IC50=30.5554 μM | SANGER | |||
| NCI-H1693 | Growth Inhibition Assay | IC50=30.5942 μM | SANGER | |||
| VM-CUB-1 | Growth Inhibition Assay | IC50=30.6413 μM | SANGER | |||
| NCI-H2170 | Growth Inhibition Assay | IC50=31.5784 μM | SANGER | |||
| ALL-PO | Growth Inhibition Assay | IC50=31.8428 μM | SANGER | |||
| NCI-H661 | Growth Inhibition Assay | IC50=32.0623 μM | SANGER | |||
| NCI-H2347 | Growth Inhibition Assay | IC50=32.4837 μM | SANGER | |||
| FTC-133 | Growth Inhibition Assay | IC50=32.706 μM | SANGER | |||
| COLO-829 | Growth Inhibition Assay | IC50=33.3467 μM | SANGER | |||
| GOTO | Growth Inhibition Assay | IC50=33.5258 μM | SANGER | |||
| YAPC | Growth Inhibition Assay | IC50=33.8159 μM | SANGER | |||
| LCLC-103H | Growth Inhibition Assay | IC50=34.1624 μM | SANGER | |||
| SiHa | Growth Inhibition Assay | IC50=34.3817 μM | SANGER | |||
| LK-2 | Growth Inhibition Assay | IC50=34.5708 μM | SANGER | |||
| KP-N-YS | Growth Inhibition Assay | IC50=34.7202 μM | SANGER | |||
| NCI-SNU-1 | Growth Inhibition Assay | IC50=35.179 μM | SANGER | |||
| KNS-81-FD | Growth Inhibition Assay | IC50=35.663 μM | SANGER | |||
| SCC-9 | Growth Inhibition Assay | IC50=36.7146 μM | SANGER | |||
| SH-4 | Growth Inhibition Assay | IC50=36.73 μM | SANGER | |||
| HCC-1954 | Growth Inhibition Assay | IC50=37.2729 μM | SANGER | |||
| BALL-1 | Growth Inhibition Assay | IC50=37.5316 μM | SANGER | |||
| BE-13 | Growth Inhibition Assay | IC50=37.7018 μM | SANGER | |||
| COLO-678 | Growth Inhibition Assay | IC50=37.9437 μM | SANGER | |||
| SK-MEL-3 | Growth Inhibition Assay | IC50=38.2397 μM | SANGER | |||
| OAW-28 | Growth Inhibition Assay | IC50=38.639 μM | SANGER | |||
| CAMA-1 | Growth Inhibition Assay | IC50=38.9691 μM | SANGER | |||
| C2BBe1 | Growth Inhibition Assay | IC50=39.818 μM | SANGER | |||
| A3-KAW | Growth Inhibition Assay | IC50=40.3661 μM | SANGER | |||
| SK-MEL-24 | Growth Inhibition Assay | IC50=40.5931 μM | SANGER | |||
| KYSE-140 | Growth Inhibition Assay | IC50=40.7165 μM | SANGER | |||
| MOLT-16 | Growth Inhibition Assay | IC50=41.1536 μM | SANGER | |||
| CFPAC-1 | Growth Inhibition Assay | IC50=42.5211 μM | SANGER | |||
| NB14 | Growth Inhibition Assay | IC50=42.7027 μM | SANGER | |||
| COLO-792 | Growth Inhibition Assay | IC50=42.8961 μM | SANGER | |||
| RH-1 | Growth Inhibition Assay | IC50=43.4836 μM | SANGER | |||
| NCI-H522 | Growth Inhibition Assay | IC50=44.3568 μM | SANGER | |||
| Ca-Ski | Growth Inhibition Assay | IC50=44.8114 μM | SANGER | |||
| KGN | Growth Inhibition Assay | IC50=48.3063 μM | SANGER | |||
| UACC-62 | Growth Inhibition Assay | IC50=48.4072 μM | SANGER | |||
| NCI-H358 | Growth Inhibition Assay | IC50=49.3018 μM | SANGER | |||
| LS-411N | Growth Inhibition Assay | IC50=49.3118 μM | SANGER | |||
| IST-MES1 | Growth Inhibition Assay | IC50=49.5625 μM | SANGER | |||
| Cliquez pour voir plus de données expérimentales sur la lignée cellulaire | ||||||
Informations chimiques, stockage et stabilité
| Poids moléculaire | 513.64 | Formule | C23H27N7O3S2 |
Stockage (À compter de la date de réception) | |
|---|---|---|---|---|---|
| N° CAS | 957054-30-7 | Télécharger le SDF | Stockage des solutions mères |
|
|
| Synonymes | RG7321 | Smiles | CS(=O)(=O)N1CCN(CC1)CC2=CC3=C(S2)C(=NC(=N3)C4=C5C=NNC5=CC=C4)N6CCOCC6 | ||
Solubilité
|
In vitro |
DMSO
: 100 mg/mL
(194.68 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 |
p110α
(Cell-free assay) 3 nM
p110δ
(Cell-free assay) 3 nM
p110β
(Cell-free assay) 33 nM
p110γ
(Cell-free assay) 75 nM
mTOR
(Cell-free assay) 0.58 μM(Ki app)
|
|---|---|
| In vitro |
Pictilisib (GDC-0941) est équipotent contre PI3Kα et PI3Kδ ainsi que contre les mutants de PI3Kα E545-K et H1047-R, affichant des niveaux de sélectivité modestes contre PI3Kβ (10 fois) et PI3Kγ (25 fois), et des niveaux de sélectivité plus élevés contre les membres des classes II, III et IV de PI3K, y compris C2β, Vps34, DNA-PK et mTOR. Il inhibe puissamment la phosphorylation d'Akt dans les cellules U87MG, PC3 et MDA-MB-361 avec des IC50 de 46 nM, 37 nM et 28 nM, respectivement. Ce composé inhibe la prolifération des cellules U87MG, A2780, PC3 et MDA-MB-361 avec des IC50 de 0,95 μM, 0,14 μM, 0,28 μM et 0,72 μM, respectivement. Il inhibe la prolifération des cellules amplifiées en HER2 qui portent des mutations PIK3CA avec une IC50 de <500 nM, et inhibe efficacement la prolifération et la viabilité des cellules de cancer du sein amplifiées en HER2. Il inhibe significativement la croissance des cellules HCT116, DLD1 et HT29 avec des GI50 de 1081 nM, 1070 nM et 157 nM, respectivement. Il inhibe également la prolifération des cellules tumorales, induit l'apoptose et supprime la population de centroblastes. |
| Essai kinase |
Essai de scintillation de proximité
|
|
Les PI3Kα, PI3Kβ et PI3Kδ recombinantes humaines sont co-exprimées dans un système de baculovirus Sf9 avec la sous-unité régulatrice p85α et purifiées sous forme de protéines de fusion GST par chromatographie d'affinité. La PI3Kγ recombinante humaine est exprimée sous forme de fusions GST monomériques et purifiée de manière similaire. Pictilisib (GDC-0941) est dissous dans du DMSO et ajouté à 20 mM de Tris-HCl (pH 7,5) contenant 200 μg de billes SPA de polylysine de silicate d'yttrium (Ysi), 4 mM de MgCl2, 1 mM de dithiothréitol (DTT), 1 μM d'ATP, 0,125 μCi de [γ-33P]-ATP et 4 % (v/v) de DMSO dans un volume total de 50 μL. La fusion GST recombinante de PI3Kα (5 ng), PI3Kβ (5 ng), PI3Kδ (5 ng) ou PI3Kγ (5 ng) est ajoutée au mélange d'essai pour initier la réaction de la kinase. Après incubation pendant 1 heure à température ambiante, la réaction de la kinase est arrêtée avec 150 μL de PBS. Le mélange est ensuite centrifugé pendant 2 minutes à 2000 tr/min et lu à l'aide d'un compteur Wallac Microbeta. Les valeurs d'IC50 rapportées sont calculées à l'aide d'une courbe dose-réponse sigmoïde ajustée dans MDL Assay Explorer.
|
|
| In vivo |
Pictilisib (GDC-0941) montre un métabolisme microsomique limité, ce qui entraîne une biodisponibilité orale de 78 % . L'administration de ce composé à 75 mg/kg/jour montre un effet inhibiteur significatif contre les xénogreffes de glioblastome humain U87MG établies chez des souris athymiques NCr femelles, avec une inhibition de la croissance tumorale de 83 %. L'administration orale de 150 mg/kg/jour inhibe la croissance des xénogreffes MDA-MB-361.1 amplifiées en HER2 chez la souris et retarde significativement la progression tumorale, en association avec une apoptose induite puissante dans les tumeurs. Le traitement avec ce composé (75 mg/kg/jour) pendant 2 semaines induit une réduction d'environ 40 % du volume tumoral des lymphomes folliculaires à cellules B spontanés développés chez les souris PTEN+/-LKB1+/hypo, accompagné d'une ablation de la phosphorylation des protéines kinases Akt, S6K et SGK (protéine kinase sérique et glucocorticoïde). |
Références |
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Applications
| Méthodes | Biomarqueurs | Images | PMID |
|---|---|---|---|
| Western blot | p-AKT / AKT / p-FoxO3a / FoxO3a / PUMA p-S6RP / S6RP p-4EBP1 / 4EBP1 p-LRP6 / LRP6 p-PAK / PAK1 / p-CRAF / RAF / p-MEK / MEK / p-ERK / ERK |
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29137323 |
| Immunofluorescence | p65 beta-catenin |
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30042442 |
| Growth inhibition assay | Cell viability |
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27117832 |
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 |
|---|---|---|---|---|---|
| NCT02092831 | Completed | Healthy Volunteer |
Genentech Inc. |
April 2014 | Phase 1 |
| NCT01740336 | Completed | Breast Cancer |
Genentech Inc. |
February 6 2013 | Phase 2 |
| NCT01474668 | Completed | Healthy Volunteer |
Genentech Inc. |
October 2011 | Phase 1 |
| NCT01240226 | Completed | Healthy Volunteer |
Genentech Inc. |
November 2010 | Phase 1 |
Support technique
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