Pictilisib (GDC-0941)
别名: RG7321
Pictilisib (GDC-0941, RG7321) 是一种有效的PI3Kα/δ抑制剂，在无细胞试验中IC50为 3 nM，对p110β (11倍)和p110γ (25倍)具有适度的选择性。Pictilisib (GDC-0941) 可诱导自噬和凋亡。Phase 2。
Pictilisib (GDC-0941) Chemical Structure
CAS: 957054-30-7
产品质控
批次：
纯度：
99.97%
99.97
Pictilisib (GDC-0941)相关产品
相关信号通路图
细胞实验数据示例
| 细胞系 | 实验类型 | 给药浓度 | 孵育时间 | 活性描述 | 文献信息 |
|---|---|---|---|---|---|
| SKOV3 | Growth Inhibition Assay | 1 μM | 96 h | GI50=0.1476 μM | 23360348 |
| MCF7 | Growth Inhibition Assay | 1 μM | 96 h | GI50=0.0702 μM | 23360348 |
| SKOV3 | Kinase Assay | 1 μM | 1 h | Inhibition of PI3Kalpha assessed as inhibition of Akt Ser473 phosphorylation | 23360348 |
| U87MG | Cytotoxic Assay | 72 h | IC50=7.77 μM | 23059545 | |
| A549 | Cytotoxic Assay | 72 h | IC50=6.9 μM | 23059545 | |
| NCI-H226 | Cytotoxic Assay | 72 h | IC50=2.9 μM | 23059545 | |
| SGC7901 | Cytotoxic Assay | 72 h | IC50=1.8 μM | 23059545 | |
| HepG2 | Cytotoxic Assay | 72 h | IC50=1 μM | 23059545 | |
| HT-29 | Cytotoxic Assay | 72 h | IC50=0.66 μM | 23059545 | |
| H460 | Cytotoxic Assay | 72 h | IC50=0.87 μM | 23059545 | |
| NCI-H1975 | Cytotoxic Assay | 72 h | IC50=0.27 μM | 23059545 | |
| MCF7.1 | Growth Inhibition Assay | 72 h | EC50=0.72 μM | 20346656 | |
| MCF7.1 | Growth Inhibition Assay | 72 h | Antiproliferative activity against human MCF7.1 cells expressing PI3Kalpha mutant with IC50 of 0.34 μM | 20050669 | |
| PC3 | Growth Inhibition Assay | 72 h | Antiproliferative activity against human PC3 cells deficient in PTEN with IC50 of 0.39 μM | 20050669 | |
| MCF7.1 | Growth Inhibition Assay | 72 h | Antiproliferative activity against human MCF7.1 cells expressing PI3Kalpha mutant with EC50 of 0.39 μM | 21985639 | |
| PC3 | Growth Inhibition Assay | 72 h | EC50=0.34 μM | 21985639 | |
| MCF7-neo/Her2 | Growth Inhibition Assay | 72 h | IC50=0.29 μM | 23662903 | |
| MCF7.1 | Growth Inhibition Assay | 72 h | Antiproliferative activity against human MCF7.1 cells expressing HER2 gene with IC50 of 0.28 μM | 21981714 | |
| PC3 | Growth Inhibition Assay | 72 h | IC50=0.28 μM | 21981714 | |
| Sf9 | Kinase Assay | 1 h | Inhibition of GST-fused human recombinant PI3Kalpha 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 PI3Kdelta expressed | 23540645 | |
| 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 | |
| RAW 264.7 | Kinase Assay | 90 min | Inhibition of human PI3Kgamma expressed assessed as inhibition of AKT phosphorylation with IC50 of 0.298 μM | 22548342 | |
| Sf9 | Kinase Assay | 30 min | Inhibition of human PI3Kgamma expressed assessed as amount of ATP consumed with IC50 of 0.042 μM | 22548342 | |
| U87MG | Growth Inhibition Assay | 96 h | IC50=0.95 μM | 18754654 | |
| PC3 | Growth Inhibition Assay | 96 h | IC50=0.28 μM | 18754654 | |
| A2780 | Growth Inhibition Assay | 96 h | Antiproliferative activity against human A2780 cells with PIK3CA and PTEN mutation with IC50 of 0.14 μM | 18754654 | |
| MDA-MB-361 | Growth Inhibition Assay | 96 h | Antiproliferative activity against human MDA-MB-361 cells with PIK3CA E545-K mutation with IC50 of 0.72 μM | 18754654 | |
| U87MG | Function Assay | 2 h | Inhibition of Akt Ser473 phosphorylation in PTEN-null human U87MG cells with IC50 of 0.046 μM | 18754654 | |
| PC3 | Function Assay | 2 h | Inhibition of Akt Ser473 phosphorylation in PTEN-null human PC3 cells with IC50 of 0.037 μM | 18754654 | |
| MDA-MB-361 | Function Assay | 2 h | Inhibition of Akt Ser473 phosphorylation in human MDA-MB-361 cells with PIK3CA E545-K mutation with IC50 of 0.028 μM | 18754654 | |
| Sf9 | Kinase Assay | 1 h | Inhibition of human recombinant PI3K p110alpha expressed in Sf9 cells coexpressing p85alpha | 18754654 | |
| Sf9 | Kinase Assay | 1 h | Inhibition of human recombinant PI3K p110beta expressed in Sf9 cells coexpressing p85alpha with IC50 of 0.033 μM | 18754654 | |
| Sf9 | Kinase Assay | 1 h | 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 | 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 | Inhibition of human recombinant PI3K p110delta expressed in Sf9 cells coexpressing p85alpha with IC50 of 0.003 μM | 18754654 | |
| HCC2157 | Growth Inhibition Assay | IC50=2.32927 μM | SANGER | ||
| D-502MG | Growth Inhibition Assay | IC50=2.32461 μM | SANGER | ||
| SF295 | Growth Inhibition Assay | IC50=2.31524 μM | SANGER | ||
| SF126 | Growth Inhibition Assay | IC50=2.30625 μM | SANGER | ||
| A431 | Growth Inhibition Assay | IC50=2.27354 μM | SANGER | ||
| EW-22 | Growth Inhibition Assay | IC50=2.25067 μM | SANGER | ||
| NCI-H2030 | Growth Inhibition Assay | IC50=2.24123 μM | SANGER | ||
| ES1 | Growth Inhibition Assay | IC50=2.21326 μM | SANGER | ||
| HCC1419 | Growth Inhibition Assay | IC50=2.21115 μM | SANGER | ||
| CHP-212 | Growth Inhibition Assay | IC50=2.18442 μM | SANGER | ||
| NCI-N87 | Growth Inhibition Assay | IC50=2.13384 μM | SANGER | ||
| KS-1 | Growth Inhibition Assay | IC50=2.11001 μM | SANGER | ||
| NCI-H1048 | Growth Inhibition Assay | IC50=2.1052 μM | SANGER | ||
| NH-12 | Growth Inhibition Assay | IC50=2.05424 μM | SANGER | ||
| LOXIMVI | Growth Inhibition Assay | IC50=2.04084 μM | SANGER | ||
| CAL-39 | Growth Inhibition Assay | IC50=2.0328 μM | SANGER | ||
| LAMA-84 | Growth Inhibition Assay | IC50=2.02689 μM | SANGER | ||
| SNB75 | Growth Inhibition Assay | IC50=2.01541 μM | SANGER | ||
| SK-MES-1 | Growth Inhibition Assay | IC50=2.01332 μM | SANGER | ||
| T98G | Growth Inhibition Assay | IC50=1.99006 μM | SANGER | ||
| HOS | Growth Inhibition Assay | IC50=1.97948 μM | SANGER | ||
| TYK-nu | Growth Inhibition Assay | IC50=1.95823 μM | SANGER | ||
| PFSK-1 | Growth Inhibition Assay | IC50=1.94458 μM | SANGER | ||
| ME-180 | Growth Inhibition Assay | IC50=1.93477 μM | SANGER | ||
| NCI-H526 | Growth Inhibition Assay | IC50=1.9139 μM | SANGER | ||
| G-402 | Growth Inhibition Assay | IC50=1.89797 μM | SANGER | ||
| BB49-HNC | Growth Inhibition Assay | IC50=1.88692 μM | SANGER | ||
| NCI-H2228 | Growth Inhibition Assay | IC50=1.85203 μM | SANGER | ||
| EW-16 | Growth Inhibition Assay | IC50=1.85182 μM | SANGER | ||
| EGI-1 | Growth Inhibition Assay | IC50=1.84701 μM | SANGER | ||
| BT-20 | Growth Inhibition Assay | IC50=1.68902 μM | SANGER | ||
| TK10 | Growth Inhibition Assay | IC50=1.67083 μM | SANGER | ||
| JVM-3 | Growth Inhibition Assay | IC50=1.64875 μM | SANGER | ||
| D-566MG | Growth Inhibition Assay | IC50=1.6253 μM | SANGER | ||
| G-401 | Growth Inhibition Assay | IC50=1.62164 μM | SANGER | ||
| EFM-19 | Growth Inhibition Assay | IC50=1.6181 μM | SANGER | ||
| VA-ES-BJ | Growth Inhibition Assay | IC50=1.6127 μM | SANGER | ||
| HuP-T4 | Growth Inhibition Assay | IC50=1.60778 μM | SANGER | ||
| Ramos-2G6-4C10 | Growth Inhibition Assay | IC50=1.60746 μM | SANGER | ||
| SK-MEL-28 | Growth Inhibition Assay | IC50=1.56085 μM | SANGER | ||
| PANC-03-27 | Growth Inhibition Assay | IC50=1.51408 μM | SANGER | ||
| A704 | Growth Inhibition Assay | IC50=1.50785 μM | SANGER | ||
| 639-V | Growth Inhibition Assay | IC50=1.50245 μM | SANGER | ||
| MDA-MB-415 | Growth Inhibition Assay | IC50=1.48692 μM | SANGER | ||
| BFTC-909 | Growth Inhibition Assay | IC50=1.43305 μM | SANGER | ||
| A549 | Growth Inhibition Assay | IC50=1.3997 μM | SANGER | ||
| Saos-2 | Growth Inhibition Assay | IC50=1.33205 μM | SANGER | ||
| AU565 | Growth Inhibition Assay | IC50=1.31863 μM | SANGER | ||
| SK-MEL-1 | Growth Inhibition Assay | IC50=1.30679 μM | SANGER | ||
| A498 | Growth Inhibition Assay | IC50=1.30474 μM | SANGER | ||
| A4-Fuk | Growth Inhibition Assay | IC50=1.29993 μM | SANGER | ||
| KYSE-270 | Growth Inhibition Assay | IC50=1.29734 μM | SANGER | ||
| LB996-RCC | Growth Inhibition Assay | IC50=1.22177 μM | SANGER | ||
| HuH-7 | Growth Inhibition Assay | IC50=1.20949 μM | SANGER | ||
| Hs-578-T | Growth Inhibition Assay | IC50=1.19565 μM | SANGER | ||
| CTB-1 | Growth Inhibition Assay | IC50=1.14293 μM | SANGER | ||
| HT | Growth Inhibition Assay | IC50=1.13478 μM | SANGER | ||
| BFTC-905 | Growth Inhibition Assay | IC50=1.13449 μM | SANGER | ||
| D-423MG | Growth Inhibition Assay | IC50=1.09962 μM | SANGER | ||
| NCI-H520 | Growth Inhibition Assay | IC50=1.08967 μM | SANGER | ||
| TGBC24TKB | Growth Inhibition Assay | IC50=1.08045 μM | SANGER | ||
| CAL-54 | Growth Inhibition Assay | IC50=1.07081 μM | SANGER | ||
| WM-115 | Growth Inhibition Assay | IC50=1.06656 μM | SANGER | ||
| SW1710 | Growth Inhibition Assay | IC50=1.04233 μM | SANGER | ||
| EKVX | Growth Inhibition Assay | IC50=1.0129 μM | SANGER | ||
| NCI-H1648 | Growth Inhibition Assay | IC50=998.51 nM | SANGER | ||
| A101D | Growth Inhibition Assay | IC50=990.19 nM | SANGER | ||
| NCI-H292 | Growth Inhibition Assay | IC50=974.32 nM | SANGER | ||
| NB5 | Growth Inhibition Assay | IC50=956.6 nM | SANGER | ||
| HDLM-2 | Growth Inhibition Assay | IC50=949.2 nM | SANGER | ||
| OVCAR-5 | Growth Inhibition Assay | IC50=940.17 nM | SANGER | ||
| NCI-H1563 | Growth Inhibition Assay | IC50=915.99 nM | SANGER | ||
| SCC-25 | Growth Inhibition Assay | IC50=914.19 nM | SANGER | ||
| MCF7 | Growth Inhibition Assay | IC50=898.59 nM | SANGER | ||
| OAW-42 | Growth Inhibition Assay | IC50=872.19 nM | SANGER | ||
| QIMR-WIL | Growth Inhibition Assay | IC50=865.2 nM | SANGER | ||
| H4 | Growth Inhibition Assay | IC50=850.85 nM | SANGER | ||
| HSC-3 | Growth Inhibition Assay | IC50=839.54 nM | SANGER | ||
| 697 | Growth Inhibition Assay | IC50=831.55 nM | SANGER | ||
| ES8 | Growth Inhibition Assay | IC50=810.52 nM | SANGER | ||
| L-363 | Growth Inhibition Assay | IC50=798.42 nM | SANGER | ||
| LNCaP-Clone-FGC | Growth Inhibition Assay | IC50=796.34 nM | SANGER | ||
| LoVo | Growth Inhibition Assay | IC50=777.9 nM | SANGER | ||
| OMC-1 | Growth Inhibition Assay | IC50=751.09 nM | SANGER | ||
| P30-OHK | Growth Inhibition Assay | IC50=730.71 nM | SANGER | ||
| SW872 | Growth Inhibition Assay | IC50=727.89 nM | SANGER | ||
| SK-NEP-1 | Growth Inhibition Assay | IC50=725.94 nM | SANGER | ||
| MV-4-11 | Growth Inhibition Assay | IC50=724.31 nM | SANGER | ||
| D-263MG | Growth Inhibition Assay | IC50=718.1 nM | SANGER | ||
| EPCL-272H | Growth Inhibition Assay | IC50=687.21 nM | SANGER | ||
| HO-1-N-1 | Growth Inhibition Assay | IC50=659.17 nM | SANGER | ||
| NEC8 | Growth Inhibition Assay | IC50=653.57 nM | SANGER | ||
| HuO-3N1 | Growth Inhibition Assay | IC50=642.38 nM | SANGER | ||
| ES4 | Growth Inhibition Assay | IC50=639.54 nM | SANGER | ||
| IGROV-1 | Growth Inhibition Assay | IC50=634.31 nM | SANGER | ||
| MOLT-4 | Growth Inhibition Assay | IC50=623.62 nM | SANGER | ||
| T47D | Growth Inhibition Assay | IC50=597.56 nM | SANGER | ||
| NKM-1 | Growth Inhibition Assay | IC50=593.09 nM | SANGER | ||
| BHT-101 | Growth Inhibition Assay | IC50=544.94 nM | SANGER | ||
| MG-63 | Growth Inhibition Assay | IC50=541.11 nM | SANGER | ||
| PA-1 | Growth Inhibition Assay | IC50=532.41 nM | SANGER | ||
| COLO-684 | Growth Inhibition Assay | IC50=523.11 nM | SANGER | ||
| LB1047-RCC | Growth Inhibition Assay | IC50=522.93 nM | SANGER | ||
| A204 | Growth Inhibition Assay | IC50=522.33 nM | SANGER | ||
| KU-19-19 | Growth Inhibition Assay | IC50=516.07 nM | SANGER | ||
| NBsusSR | Growth Inhibition Assay | IC50=488.85 nM | SANGER | ||
| LXF-289 | Growth Inhibition Assay | IC50=448.27 nM | SANGER | ||
| MDA-MB-361 | Growth Inhibition Assay | IC50=439.13 nM | SANGER | ||
| GCIY | Growth Inhibition Assay | IC50=433.8 nM | SANGER | ||
| HL-60 | Growth Inhibition Assay | IC50=425.75 nM | SANGER | ||
| MFE-280 | Growth Inhibition Assay | IC50=418.2 nM | SANGER | ||
| NB7 | Growth Inhibition Assay | IC50=389.83 nM | SANGER | ||
| CHL-1 | Growth Inhibition Assay | IC50=378.65 nM | SANGER | ||
| GAMG | Growth Inhibition Assay | IC50=370.85 nM | SANGER | ||
| MDA-MB-175-VII | Growth Inhibition Assay | IC50=352.92 nM | SANGER | ||
| ES7 | Growth Inhibition Assay | IC50=341.99 nM | SANGER | ||
| AN3-CA | Growth Inhibition Assay | IC50=340.37 nM | SANGER | ||
| BPH-1 | Growth Inhibition Assay | IC50=314 nM | SANGER | ||
| YH-13 | Growth Inhibition Assay | IC50=304.32 nM | SANGER | ||
| NCI-H1623 | Growth Inhibition Assay | IC50=304.08 nM | SANGER | ||
| LB2241-RCC | Growth Inhibition Assay | IC50=303.84 nM | SANGER | ||
| DOK | Growth Inhibition Assay | IC50=301.7 nM | SANGER | ||
| RS4-11 | Growth Inhibition Assay | IC50=261.76 nM | SANGER | ||
| NB69 | Growth Inhibition Assay | IC50=245.27 nM | SANGER | ||
| HGC-27 | Growth Inhibition Assay | IC50=212.57 nM | SANGER | ||
| NOS-1 | Growth Inhibition Assay | IC50=211.82 nM | SANGER | ||
| HAL-01 | Growth Inhibition Assay | IC50=206.73 nM | SANGER | ||
| HuO9 | Growth Inhibition Assay | IC50=206.02 nM | SANGER | ||
| NCI-H1770 | Growth Inhibition Assay | IC50=123.86 nM | SANGER | ||
| MHH-PREB-1 | Growth Inhibition Assay | IC50=114.3 nM | SANGER | ||
| HH | Growth Inhibition Assay | IC50=111.08 nM | SANGER | ||
| ES5 | Growth Inhibition Assay | IC50=50.21 nM | SANGER | ||
| PC3 | Growth Inhibition Assay | logGI50=-6.66 M | 22336246 | ||
| DU145 | Growth Inhibition Assay | logGI50=-5.85 M | 22336246 | ||
| MKN74 | Growth Inhibition Assay | logGI50=-6.02 M | 22336246 | ||
| MKN45 | Growth Inhibition Assay | logGI50=-6.55 M | 22336246 | ||
| MKN28 | Growth Inhibition Assay | logGI50=-5.52 M | 22336246 | ||
| MKN7 | Growth Inhibition Assay | logGI50=-6.50 M | 22336246 | ||
| MKN1 | Growth Inhibition Assay | logGI50=-7.08 M | 22336246 | ||
| St-4 | Growth Inhibition Assay | logGI50=-5.56 M | 22336246 | ||
| ACHN | Growth Inhibition Assay | logGI50=-6.07 M | 22336246 | ||
| RXF631L | Growth Inhibition Assay | logGI50=-6.88 M | 22336246 | ||
| SKOV3 | Growth Inhibition Assay | logGI50=-6.52 M | 22336246 | ||
| OVCAR8 | Growth Inhibition Assay | logGI50=-5.73 M | 22336246 | ||
| OVCAR5 | Growth Inhibition Assay | logGI50=-6.26 M | 22336246 | ||
| OVCAR4 | Growth Inhibition Assay | logGI50=-5.76 M | 22336246 | ||
| OVCAR3 | Growth Inhibition Assay | logGI50=-6.71 M | 22336246 | ||
| LOXIMVI | Growth Inhibition Assay | logGI50=-6.29 M | 22336246 | ||
| DMS114 | Growth Inhibition Assay | logGI50=-5.92 M | 22336246 | ||
| DMS273 | Growth Inhibition Assay | logGI50=-6.43 M | 22336246 | ||
| A549 | Growth Inhibition Assay | logGI50=-6.15 M | 22336246 | ||
| NCI-H483 | Growth Inhibition Assay | logGI50=-6.56 M | 22336246 | ||
| NCI-H522 | Growth Inhibition Assay | logGI50=-6.58 M | 22336246 | ||
| NCI-H226 | Growth Inhibition Assay | logGI50=-6.21 M | 22336246 | ||
| NCI-H23 | Growth Inhibition Assay | logGI50=-5.73 M | 22336246 | ||
| HCT116 | Growth Inhibition Assay | logGI50=-5.87 M | 22336246 | ||
| HCT15 | Growth Inhibition Assay | logGI50=-6.12 M | 22336246 | ||
| HT-29 | Growth Inhibition Assay | logGI50=-6.30 M | 22336246 | ||
| KM12 | Growth Inhibition Assay | logGI50=-5.76 M | 22336246 | ||
| HCC2998 | Growth Inhibition Assay | logGI50=-6.29 M | 22336246 | ||
| SNB78 | Growth Inhibition Assay | logGI50=-6.52 M | 22336246 | ||
| SNB75 | Growth Inhibition Assay | logGI50=-7.10 M | 22336246 | ||
| SF539 | Growth Inhibition Assay | logGI50=-6.50 M | 22336246 | ||
| SF295 | Growth Inhibition Assay | logGI50=-6.37 M | 22336246 | ||
| SF268 | Growth Inhibition Assay | logGI50=-5.39 M | 22336246 | ||
| U251 | Growth Inhibition Assay | logGI50=-5.50 M | 22336246 | ||
| MDA-MB-231 | Growth Inhibition Assay | logGI50=-5.46 M | 22336246 | ||
| MCF7 | Growth Inhibition Assay | logGI50=-7.33 M | 22336246 | ||
| HBC5 | Growth Inhibition Assay | logGI50=-6.60 M | 22336246 | ||
| BSY1 | Growth Inhibition Assay | logGI50=-6.90 M | 22336246 | ||
| HBC4 | Growth Inhibition Assay | logGI50=-6.03 M | 22336246 | ||
| MCF7-neo/Her2 | Kinase Assay | Inhibition of PI3Kalpha assessed as reduction of AKT phosphorylation at S473 with IC50 of 0.007 μM | 23662903 | ||
| 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 | ||
| 点击查看更多细胞系数据 | |||||
生物活性
| 产品描述 | Pictilisib (GDC-0941, RG7321) 是一种有效的PI3Kα/δ抑制剂，在无细胞试验中IC50为 3 nM，对p110β (11倍)和p110γ (25倍)具有适度的选择性。Pictilisib (GDC-0941) 可诱导自噬和凋亡。Phase 2。 | ||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|
| 靶点 |
|
| 体外研究(In Vitro) | ||||
| 体外研究活性 | GDC-0941也等效作用于PI3Kα和 PI3Kδ和PI3Kα突变型E545-K和H1047-R,也选择性作用于PI3Kβ(10倍)和 PI3Kγ(25倍), 选择性更高地作用于PI3K II, III, 和IV类成员，包括, C2β, Vps34, DNA-PK和mTOR。GDC-0941 作用于U87MG, PC3, 和 MDA-MB-361 细胞，有效抑制Akt磷酸化，IC50分别为46 nM, 37 nM,和 28 nM。GDC-0941抑制U87MG, A2780, PC3, 和MDA-MB-361细胞增殖，IC50分别为 0.95 μM, 0.14 μM, 0.28 μM, 和0.72 μM。[1]GDC-0941抑制含PIK3CA突变的HER2扩增的细胞增殖，IC50<500 nM, 且有效抑制HER2 扩增乳腺癌细胞增殖和活力。[2]GDC-0941 显著抑制HCT116, DLD1和 HT29细胞生长，GI50分别为1081 nM, 1070 nM 和157 nM。[4] |
|||
|---|---|---|---|---|
| 激酶实验 | 闪烁接近检测 | |||
| 使用p85α调节亚基，使重组人PI3Kα, PI3Kβ, 和PI3Kδ在 Sf9 杆状病毒系统中共表达，在谷胱甘肽-琼脂糖凝胶上进行亲和层析而纯化GST-融合蛋白。重组人 PI3Kγ表达作为单体 GST融合，也想上述相似方法纯化。GDC-0941 溶于DMSO，加到含200 μg硅酸钇(Ysi) 聚赖氨酸SPA 磁珠, 4 mM MgCl2, 1 mM 二硫苏糖醇 (DTT), 1 μM ATP, 0.125 μCi [γ-33P]-ATP, 和4% (v/v) DMSO的20 mM Tris-HCl (pH 7.5)上，总体积为 50 μL。PI3Kα (5 ng), PI3Kβ(5 ng), PI3Kδ(5 ng), 或PI3Kγ(5 ng)的重组GST-融合 ，加到实验混合物中，开始激酶反应。在室温下温育1小时后, 加入150 μL PBS终止反应。混合物在2000 rpm 转速下离心2分钟，然后使用Wallac Microbeta计数器读数。在 MDL Assay Explorer系统中使用S型，剂量-反应曲线，计算进行至少2次独立重复实验，取平均值，作为IC50值。 | ||||
| 细胞实验 | 细胞系 | SKBR-3, BT474-M1, AU-565, HCC-1419, ZR75-30, KPL-4, JIMT-1, BT474-EEI, HCC-1954, MCF-7, CALU-3, SKOV-3, 和MKN-7 | ||
| 浓度 | 溶于DMSO,终浓度为~10 μM | |||
| 孵育时间 | 48,和72小时 | |||
| 方法 | 使用不同浓度 GDC-0941处理细胞48,和 72小时。通过CellTiter-Glo Luminescent细胞活性检测实验测定细胞增殖/活力。通过Western Blot分析pAKT (Ser473), cleaved caspase-3, 和cleaved PARP通过 Caspase-Glo 3/7实验和细胞死亡检测 ELISAplus 实验分别测定caspase 3/7活性, 和凋亡。 |
|||
| 实验图片 | 检测方法 | 检测指标 | 实验图片 | 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 |
|
29137323 | |
| Immunofluorescence | p65 beta-catenin |
|
30042442 | |
| Growth inhibition assay | Cell viability |
|
27117832 | |
| 体内研究(In Vivo) | ||
| 体内研究活性 | 在微粒体中，GDC-0941仅有有限的代谢，其口服生物利用度为78%[5]。GDC-0941 每天按 75 mg/kg剂量处理携带人U87MG 恶性胶质移植瘤的雌性NCr无胸腺小鼠，显著抑制生长，肿瘤生长抑制率为 83%。[1]GDC-0941 每天按 150 mg/kg剂量口服处理携带HER2扩增的MDA-MB-361.1移植瘤 的小鼠，抑制肿瘤生长，且显著延迟肿瘤衰退，与肿瘤中强诱导型凋亡相关。[2] GDC-0941 每天按75 mg/kg剂量处理携带自发性B细胞滤泡性淋巴瘤的PTEN+/-LKB1+/hypo小鼠，持续2周，诱导肿瘤体积下降~40%，伴随着AKT, S6K 和SGK(血清和糖皮质激素蛋白激酶)蛋白激酶的磷酸化被切除。GDC-0941抑制肿瘤细胞增殖，诱导凋亡和抑制中心母细胞数。[3] |
|
|---|---|---|
| 动物实验 | Animal Models | 移植MDA-MB-361.1细胞的NCR裸鼠, 皮下移植BT474-M1 细胞的SCID, C.B-17/IcrHsd-Prkdcscid 小鼠 |
| Dosages | ~150 mg/kg/day | |
| Administration | 口服饲喂 | |
| NCT Number | Recruitment | Conditions | Sponsor/Collaborators | Start Date | 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 |
化学信息&溶解度
| 分子量 | 513.64 | 分子式 | C23H27N7O3S2 |
| CAS号 | 957054-30-7 | SDF | Download Pictilisib (GDC-0941) SDF |
| Smiles | CS(=O)(=O)N1CCN(CC1)CC2=CC3=C(S2)C(=NC(=N3)C4=C5C=NNC5=CC=C4)N6CCOCC6 | ||
| 储存条件(自收到货起) | |||
|
体外溶解度 |
DMSO : 100 mg/mL ( (194.68 mM) ；DMSO吸湿会降低化合物溶解度，请使用新开封DMSO) Water : Insoluble Ethanol : Insoluble |
摩尔浓度计算器 |
|
体内溶解度 现配现用，请按从左到右的顺序依次添加，澄清后再加入下一溶剂 |
动物体内配方计算器 | ||||
实验计算
动物体内配方计算器（澄清溶液）
第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量）
mg/kg
g
μL
只
第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系Selleck为您提供正确的澄清溶液配方）
% DMSO
%
% Tween 80
% ddH2O
%DMSO
%
计算结果：
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于μL DMSO溶液（母液浓度mg/mL，注：如该浓度超过该批次药物DMSO溶解度，请先联系Selleck）；
体内配方配制方法：取μL DMSO母液，加入μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入μL ddH2O，混匀澄清。
体内配方配制方法：取μL DMSO母液，加入μL Corn oil，混匀澄清。
注意：1. 首先保证母液是澄清的；
2.一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
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