Dactolisib (BEZ235)
别名: NVP-BEZ235
Dactolisib (BEZ235, NVP-BEZ235) 是一种双重ATP竞争性 PI3K 和 mTOR 抑制剂，在无细胞试验中，抑制 p110α/γ/δ/β 和 mTOR(p70S6K) 的 IC50 分别为 4 nM /5 nM /7 nM /75 nM /6 nM。 在 3T3TopBP1-ER 细胞中抑制 ATR，IC50 为 21 nM，而对 Akt 和 PDK1 的抑制作用很弱。Dactolisib可诱导自噬并抑制HIV-1的复制。Phase 2。
Dactolisib (BEZ235) Chemical Structure
CAS: 915019-65-7
产品质控
批次：
纯度：
99.99%
99.99
Dactolisib (BEZ235)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 |
|---|---|---|---|---|---|
| Trypanosoma brucei brucei | Function Assay | 200 nM | 12 h | Effect on phosphatidylcholine level | 24805946 |
| Trypanosoma brucei brucei | Function Assay | 200 nM | 12 h | Effect on sphingomylein level | 24805946 |
| Trypanosoma brucei brucei | Function Assay | 200 nM | 12 h | Decrease in phosphotidyl inositol phosphate level | 24805946 |
| PC3 | Growth Inhibition Assay | 0.01-100 μM | 48 h | Log GI50=-8.66 M | 22336246 |
| DU145 | Growth Inhibition Assay | 0.01-100 μM | 48 h | Log GI50=-8.16 M | 22336246 |
| MKN74 | Growth Inhibition Assay | 0.01-100 μM | 48 h | Log GI50=-7.42 M | 22336246 |
| MKN45 | Growth Inhibition Assay | 0.01-100 μM | 48 h | Log GI50=-8.34 M | 22336246 |
| MKN28 | Growth Inhibition Assay | 0.01-100 μM | 48 h | Log GI50=-7.07 M | 22336246 |
| MKN7 | Growth Inhibition Assay | 0.01-100 μM | 48 h | Log GI50=-7.68 M | 22336246 |
| MKN1 | Growth Inhibition Assay | 0.01-100 μM | 48 h | Log GI50=-8.41 M | 22336246 |
| St-4 | Growth Inhibition Assay | 0.01-100 μM | 48 h | Log GI50=-7.47 M | 22336246 |
| ACHN | Growth Inhibition Assay | 0.01-100 μM | 48 h | Log GI50=-7.95 M | 22336246 |
| RXF631L | Growth Inhibition Assay | 0.01-100 μM | 48 h | Log GI50=-8.21 M | 22336246 |
| SKOV3 | Growth Inhibition Assay | 0.01-100 μM | 48 h | Log GI50=-8.41 M | 22336246 |
| OVCAR8 | Growth Inhibition Assay | 0.01-100 μM | 48 h | Log GI50=-7.84 M | 22336246 |
| OVCAR5 | Growth Inhibition Assay | 0.01-100 μM | 48 h | Log GI50=-7.57 M | 22336246 |
| OVCAR4 | Growth Inhibition Assay | 0.01-100 μM | 48 h | Log GI50=-8.58 M | 22336246 |
| OVCAR3 | Growth Inhibition Assay | 0.01-100 μM | 48 h | Log GI50=-8.17 M | 22336246 |
| LOXIMVI | Growth Inhibition Assay | 0.01-100 μM | 48 h | Log GI50=-8.66 M | 22336246 |
| DMS114 | Growth Inhibition Assay | 0.01-100 μM | 48 h | Log GI50=-8.39 M | 22336246 |
| DMS273 | Growth Inhibition Assay | 0.01-100 μM | 48 h | Log GI50=-7.80 M | 22336246 |
| A549 | Growth Inhibition Assay | 0.01-100 μM | 48 h | Log GI50=-8.07 M | 22336246 |
| NCI-H438 | Growth Inhibition Assay | 0.01-100 μM | 48 h | Log GI50=-8.11 M | 22336246 |
| NCI-H522 | Growth Inhibition Assay | 0.01-100 μM | 48 h | Log GI50=-8.45 M | 22336246 |
| NCI-H226 | Growth Inhibition Assay | 0.01-100 μM | 48 h | Log GI50=-8.44 M | 22336246 |
| NCI-H23 | Growth Inhibition Assay | 0.01-100 μM | 48 h | Log GI50=-7.64 M | 22336246 |
| HCT116 | Growth Inhibition Assay | 0.01-100 μM | 48 h | Log GI50=-7.61 M | 22336246 |
| HCT15 | Growth Inhibition Assay | 0.01-100 μM | 48 h | Log GI50=-8.03 M | 22336246 |
| HT-29 | Growth Inhibition Assay | 0.01-100 μM | 48 h | Log GI50=-7.75 M | 22336246 |
| KM12 | Growth Inhibition Assay | 0.01-100 μM | 48 h | Log GI50=-7.54 M | 22336246 |
| HCC2998 | Growth Inhibition Assay | 0.01-100 μM | 48 h | Log GI50=-8.05 M | 22336246 |
| SNB78 | Growth Inhibition Assay | 0.01-100 μM | 48 h | Log GI50=-8.65 M | 22336246 |
| SNB75 | Growth Inhibition Assay | 0.01-100 μM | 48 h | Log GI50=-8.58 M | 22336246 |
| SF539 | Growth Inhibition Assay | 0.01-100 μM | 48 h | Log GI50=-8.59 M | 22336246 |
| SF295 | Growth Inhibition Assay | 0.01-100 μM | 48 h | Log GI50=-8.31 M | 22336246 |
| SF268 | Growth Inhibition Assay | 0.01-100 μM | 48 h | Log GI50=-7.92 M | 22336246 |
| U251 | Growth Inhibition Assay | 0.01-100 μM | 48 h | Log GI50=-7.66 M | 22336246 |
| MDA-MB-231 | Growth Inhibition Assay | 0.01-100 μM | 48 h | Log GI50=-8.09 M | 22336246 |
| MCF7 | Growth Inhibition Assay | 0.01-100 μM | 48 h | Log GI50=-8.16 M | 22336246 |
| HBC5 | Growth Inhibition Assay | 0.01-100 μM | 48 h | Log GI50=-7.87 M | 22336246 |
| BSY1 | Growth Inhibition Assay | 0.01-100 μM | 48 h | Log GI50=-8.48 M | 22336246 |
| HBC4 | Growth Inhibition Assay | 0.01-100 μM | 48 h | Log GI50=-8.61 M | 22336246 |
| U87MG | Growth Inhibition Assay | 0.01-100 μM | 48 h | IC50=1.32 μM | 23871904 |
| HCT116 | Growth Inhibition Assay | 0.01-100 μM | 48 h | IC50=1.16 μM | 23871904 |
| MCF7 | Growth Inhibition Assay | 0.01-100 μM | 48 h | IC50=0.73 μM | 23871904 |
| Trypanosoma brucei brucei | Function Assay | 18 h | Inhibition of receptor-mediated endocytosis assessed as decrease in transferrin uptake | 24805946 | |
| Trypanosoma brucei brucei | Antimicrobial Assay | 18 h | Antitrypanosomal activity with EC50 of 0.0025 μM | 24805946 | |
| AGS | Growth Inhibition Assay | IC50=48.77 nM | SANGER | ||
| MCF7 | Growth Inhibition Assay | IC50=48.58 nM | SANGER | ||
| LoVo | Growth Inhibition Assay | IC50=48.4 nM | SANGER | ||
| NCI-H1155 | Growth Inhibition Assay | IC50=48.32 nM | SANGER | ||
| NCI-H1623 | Growth Inhibition Assay | IC50=47.76 nM | SANGER | ||
| LB996-RCC | Growth Inhibition Assay | IC50=47.19 nM | SANGER | ||
| TE-5 | Growth Inhibition Assay | IC50=46.84 nM | SANGER | ||
| PC-14 | Growth Inhibition Assay | IC50=46.57 nM | SANGER | ||
| A4-Fuk | Growth Inhibition Assay | IC50=46.52 nM | SANGER | ||
| DOHH-2 | Growth Inhibition Assay | IC50=46.37 nM | SANGER | ||
| NCI-H1355 | Growth Inhibition Assay | IC50=46.34 nM | SANGER | ||
| EW-22 | Growth Inhibition Assay | IC50=46.2 nM | SANGER | ||
| KYSE-180 | Growth Inhibition Assay | IC50=46.17 nM | SANGER | ||
| IGR-1 | Growth Inhibition Assay | IC50=46.13 nM | SANGER | ||
| SK-HEP-1 | Growth Inhibition Assay | IC50=46.04 nM | SANGER | ||
| NOMO-1 | Growth Inhibition Assay | IC50=45.87 nM | SANGER | ||
| KNS-62 | Growth Inhibition Assay | IC50=45.38 nM | SANGER | ||
| HD-MY-Z | Growth Inhibition Assay | IC50=44.92 nM | SANGER | ||
| KS-1 | Growth Inhibition Assay | IC50=44.66 nM | SANGER | ||
| NCI-H2452 | Growth Inhibition Assay | IC50=44.58 nM | SANGER | ||
| PSN1 | Growth Inhibition Assay | IC50=44.4 nM | SANGER | ||
| EPLC-272H | Growth Inhibition Assay | IC50=44.39 nM | SANGER | ||
| T-24 | Growth Inhibition Assay | IC50=43.83 nM | SANGER | ||
| NTERA-S-cl-D1 | Growth Inhibition Assay | IC50=43 nM | SANGER | ||
| BHY | Growth Inhibition Assay | IC50=42.72 nM | SANGER | ||
| 8305C | Growth Inhibition Assay | IC50=41.87 nM | SANGER | ||
| HT | Growth Inhibition Assay | IC50=41.02 nM | SANGER | ||
| G-401 | Growth Inhibition Assay | IC50=40.82 nM | SANGER | ||
| NB5 | Growth Inhibition Assay | IC50=40.64 nM | SANGER | ||
| MZ2-MEL | Growth Inhibition Assay | IC50=39.66 nM | SANGER | ||
| MDA-MB-175-VII | Growth Inhibition Assay | IC50=39.51 nM | SANGER | ||
| A101D | Growth Inhibition Assay | IC50=38.97 nM | SANGER | ||
| LB1047-RCC | Growth Inhibition Assay | IC50=38.81 nM | SANGER | ||
| CO-314 | Growth Inhibition Assay | IC50=38.74 nM | SANGER | ||
| HCC1419 | Growth Inhibition Assay | IC50=38.71 nM | SANGER | ||
| CAL-12T | Growth Inhibition Assay | IC50=38.6 nM | SANGER | ||
| SJSA-1 | Growth Inhibition Assay | IC50=38.54 nM | SANGER | ||
| U251 | Growth Inhibition Assay | IC50=38.43 nM | SANGER | ||
| RKO | Growth Inhibition Assay | IC50=38.33 nM | SANGER | ||
| MN-60 | Growth Inhibition Assay | IC50=37.96 nM | SANGER | ||
| CAL-39 | Growth Inhibition Assay | IC50=37.9 nM | SANGER | ||
| LNCaP-Clone-FGC | Growth Inhibition Assay | IC50=37.59 nM | SANGER | ||
| 8505C | Growth Inhibition Assay | IC50=37.51 nM | SANGER | ||
| 8-MG-BA | Growth Inhibition Assay | IC50=37.25 nM | SANGER | ||
| CAL-62 | Growth Inhibition Assay | IC50=36.86 nM | SANGER | ||
| Daoy | Growth Inhibition Assay | IC50=36.7 nM | SANGER | ||
| CAKI-1 | Growth Inhibition Assay | IC50=36.43 nM | SANGER | ||
| LAMA-84 | Growth Inhibition Assay | IC50=35.87 nM | SANGER | ||
| OVCAR-5 | Growth Inhibition Assay | IC50=35.47 nM | SANGER | ||
| MDA-MB-157 | Growth Inhibition Assay | IC50=35.41 nM | SANGER | ||
| CAL-120 | Growth Inhibition Assay | IC50=34.72 nM | SANGER | ||
| NCI-H28 | Growth Inhibition Assay | IC50=34.44 nM | SANGER | ||
| Becker | Growth Inhibition Assay | IC50=34.21 nM | SANGER | ||
| SK-NEP-1 | Growth Inhibition Assay | IC50=34.15 nM | SANGER | ||
| RPMI-8226 | Growth Inhibition Assay | IC50=33.82 nM | SANGER | ||
| COLO-684 | Growth Inhibition Assay | IC50=33.58 nM | SANGER | ||
| Ca9-22 | Growth Inhibition Assay | IC50=33.55 nM | SANGER | ||
| VM-CUB-1 | Growth Inhibition Assay | IC50=33.43 nM | SANGER | ||
| A2058 | Growth Inhibition Assay | IC50=33.25 nM | SANGER | ||
| COLO-800 | Growth Inhibition Assay | IC50=32.92 nM | SANGER | ||
| CTV-1 | Growth Inhibition Assay | IC50=32.82 nM | SANGER | ||
| ECC10 | Growth Inhibition Assay | IC50=31.95 nM | SANGER | ||
| EW-18 | Growth Inhibition Assay | IC50=31.86 nM | SANGER | ||
| BE-13 | Growth Inhibition Assay | IC50=31.82 nM | SANGER | ||
| BEN | Growth Inhibition Assay | IC50=31.63 nM | SANGER | ||
| OVCAR-8 | Growth Inhibition Assay | IC50=31.26 nM | SANGER | ||
| KU-19-19 | Growth Inhibition Assay | IC50=31.13 nM | SANGER | ||
| JVM-3 | Growth Inhibition Assay | IC50=30.83 nM | SANGER | ||
| QIMR-WIL | Growth Inhibition Assay | IC50=30.6 nM | SANGER | ||
| AsPC-1 | Growth Inhibition Assay | IC50=30.2 nM | SANGER | ||
| NOS-1 | Growth Inhibition Assay | IC50=30.12 nM | SANGER | ||
| BHT-101 | Growth Inhibition Assay | IC50=30.05 nM | SANGER | ||
| GI-ME-N | Growth Inhibition Assay | IC50=29.91 nM | SANGER | ||
| T98G | Growth Inhibition Assay | IC50=29.88 nM | SANGER | ||
| U-2-OS | Growth Inhibition Assay | IC50=29.5 nM | SANGER | ||
| D-263MG | Growth Inhibition Assay | IC50=29.35 nM | SANGER | ||
| ONS-76 | Growth Inhibition Assay | IC50=29.05 nM | SANGER | ||
| ES1 | Growth Inhibition Assay | IC50=28.84 nM | SANGER | ||
| MV-4-11 | Growth Inhibition Assay | IC50=28.7 nM | SANGER | ||
| A3-KAW | Growth Inhibition Assay | IC50=28.64 nM | SANGER | ||
| A204 | Growth Inhibition Assay | IC50=28.47 nM | SANGER | ||
| SW1088 | Growth Inhibition Assay | IC50=28.29 nM | SANGER | ||
| DB | Growth Inhibition Assay | IC50=27.36 nM | SANGER | ||
| NCI-H292 | Growth Inhibition Assay | IC50=27 nM | SANGER | ||
| RS4-11 | Growth Inhibition Assay | IC50=26.91 nM | SANGER | ||
| SW962 | Growth Inhibition Assay | IC50=26.76 nM | SANGER | ||
| HuO9 | Growth Inhibition Assay | IC50=26.76 nM | SANGER | ||
| HOP-92 | Growth Inhibition Assay | IC50=26.48 nM | SANGER | ||
| SK-LU-1 | Growth Inhibition Assay | IC50=26.17 nM | SANGER | ||
| LXF-289 | Growth Inhibition Assay | IC50=26.04 nM | SANGER | ||
| KYSE-150 | Growth Inhibition Assay | IC50=25.89 nM | SANGER | ||
| MPP-89 | Growth Inhibition Assay | IC50=25.32 nM | SANGER | ||
| TI-73 | Growth Inhibition Assay | IC50=25.28 nM | SANGER | ||
| ES3 | Growth Inhibition Assay | IC50=25.22 nM | SANGER | ||
| HO-1-N-1 | Growth Inhibition Assay | IC50=25.15 nM | SANGER | ||
| MOLT-4 | Growth Inhibition Assay | IC50=25.12 nM | SANGER | ||
| FTC-133 | Growth Inhibition Assay | IC50=25.1 nM | SANGER | ||
| CTB-1 | Growth Inhibition Assay | IC50=24.67 nM | SANGER | ||
| NBsusSR | Growth Inhibition Assay | IC50=24.6 nM | SANGER | ||
| Hs-578-T | Growth Inhibition Assay | IC50=24.58 nM | SANGER | ||
| EFO-27 | Growth Inhibition Assay | IC50=24.33 nM | SANGER | ||
| MEL-HO | Growth Inhibition Assay | IC50=24.04 nM | SANGER | ||
| A375 | Growth Inhibition Assay | IC50=23.93 nM | SANGER | ||
| CAL-51 | Growth Inhibition Assay | IC50=23.89 nM | SANGER | ||
| BV-173 | Growth Inhibition Assay | IC50=23.87 nM | SANGER | ||
| MG-63 | Growth Inhibition Assay | IC50=23.45 nM | SANGER | ||
| SW780 | Growth Inhibition Assay | IC50=23.13 nM | SANGER | ||
| TGBC1TKB | Growth Inhibition Assay | IC50=23.05 nM | SANGER | ||
| J-RT3-T3-5 | Growth Inhibition Assay | IC50=22.96 nM | SANGER | ||
| NB69 | Growth Inhibition Assay | IC50=22.53 nM | SANGER | ||
| ME-180 | Growth Inhibition Assay | IC50=22.43 nM | SANGER | ||
| 786-0 | Growth Inhibition Assay | IC50=22.29 nM | SANGER | ||
| G-402 | Growth Inhibition Assay | IC50=22.16 nM | SANGER | ||
| NCI-SNU-1 | Growth Inhibition Assay | IC50=21.95 nM | SANGER | ||
| HT-1080 | Growth Inhibition Assay | IC50=21.93 nM | SANGER | ||
| YH-13 | Growth Inhibition Assay | IC50=21.88 nM | SANGER | ||
| NCI-H2030 | Growth Inhibition Assay | IC50=21.52 nM | SANGER | ||
| RXF393 | Growth Inhibition Assay | IC50=21.45 nM | SANGER | ||
| ES4 | Growth Inhibition Assay | IC50=21.08 nM | SANGER | ||
| HOS | Growth Inhibition Assay | IC50=21.06 nM | SANGER | ||
| CGTH-W-1 | Growth Inhibition Assay | IC50=20.63 nM | SANGER | ||
| DEL | Growth Inhibition Assay | IC50=20.49 nM | SANGER | ||
| RT-112 | Growth Inhibition Assay | IC50=19.66 nM | SANGER | ||
| KNS-81-FD | Growth Inhibition Assay | IC50=19.54 nM | SANGER | ||
| GAMG | Growth Inhibition Assay | IC50=19.48 nM | SANGER | ||
| SF126 | Growth Inhibition Assay | IC50=19.41 nM | SANGER | ||
| RPMI-7951 | Growth Inhibition Assay | IC50=19.28 nM | SANGER | ||
| SF295 | Growth Inhibition Assay | IC50=18.93 nM | SANGER | ||
| IST-MEL1 | Growth Inhibition Assay | IC50=18.77 nM | SANGER | ||
| SW1710 | Growth Inhibition Assay | IC50=18.72 nM | SANGER | ||
| BCPAP | Growth Inhibition Assay | IC50=18.65 nM | SANGER | ||
| HuH-7 | Growth Inhibition Assay | IC50=18.4 nM | SANGER | ||
| ES7 | Growth Inhibition Assay | IC50=18.09 nM | SANGER | ||
| HGC-27 | Growth Inhibition Assay | IC50=18.06 nM | SANGER | ||
| EW-16 | Growth Inhibition Assay | IC50=18.04 nM | SANGER | ||
| VA-ES-BJ | Growth Inhibition Assay | IC50=17.83 nM | SANGER | ||
| D-56MG | Growth Inhibition Assay | IC50=17.69 nM | SANGER | ||
| 697 | Growth Inhibition Assay | IC50=17.43 nM | SANGER | ||
| NCI-H209 | Growth Inhibition Assay | IC50=17.29 nM | SANGER | ||
| MOLT-16 | Growth Inhibition Assay | IC50=17.15 nM | SANGER | ||
| OS-RC-2 | Growth Inhibition Assay | IC50=16.47 nM | SANGER | ||
| EGI-1 | Growth Inhibition Assay | IC50=16.43 nM | SANGER | ||
| NUGC-3 | Growth Inhibition Assay | IC50=16.34 nM | SANGER | ||
| HH | Growth Inhibition Assay | IC50=15.7 nM | SANGER | ||
| VMRC-RCZ | Growth Inhibition Assay | IC50=15.63 nM | SANGER | ||
| CHL-1 | Growth Inhibition Assay | IC50=15.45 nM | SANGER | ||
| P12-ICHIKAWA | Growth Inhibition Assay | IC50=15.1 nM | SANGER | ||
| COR-L105 | Growth Inhibition Assay | IC50=15.04 nM | SANGER | ||
| LOXIMVI | Growth Inhibition Assay | IC50=14.99 nM | SANGER | ||
| ES5 | Growth Inhibition Assay | IC50=14.74 nM | SANGER | ||
| LB2241-RCC | Growth Inhibition Assay | IC50=14.01 nM | SANGER | ||
| EoL-1 | Growth Inhibition Assay | IC50=13.93 nM | SANGER | ||
| GCT | Growth Inhibition Assay | IC50=13.68 nM | SANGER | ||
| KARPAS-45 | Growth Inhibition Assay | IC50=13.51 nM | SANGER | ||
| NCI-H1793 | Growth Inhibition Assay | IC50=12.82 nM | SANGER | ||
| BB65-RCC | Growth Inhibition Assay | IC50=12.72 nM | SANGER | ||
| H4 | Growth Inhibition Assay | IC50=12.67 nM | SANGER | ||
| HSC-3 | Growth Inhibition Assay | IC50=12.21 nM | SANGER | ||
| Mewo | Growth Inhibition Assay | IC50=11.99 nM | SANGER | ||
| PA-1 | Growth Inhibition Assay | IC50=11.82 nM | SANGER | ||
| ES8 | Growth Inhibition Assay | IC50=10.9 nM | SANGER | ||
| L-363 | Growth Inhibition Assay | IC50=10.69 nM | SANGER | ||
| 769-P | Growth Inhibition Assay | IC50=10.44 nM | SANGER | ||
| A549 | Growth Inhibition Assay | IC50=10.14 nM | SANGER | ||
| MFE-280 | Growth Inhibition Assay | IC50=9.99 nM | SANGER | ||
| TYK-nu | Growth Inhibition Assay | IC50=9.94 nM | SANGER | ||
| CAMA-1 | Growth Inhibition Assay | IC50=9.8 nM | SANGER | ||
| NCI-H1666 | Growth Inhibition Assay | IC50=9.71 nM | SANGER | ||
| DU-4475 | Growth Inhibition Assay | IC50=9.44 nM | SANGER | ||
| MHH-PREB-1 | Growth Inhibition Assay | IC50=9.12 nM | SANGER | ||
| Ramos-2G6-4C10 | Growth Inhibition Assay | IC50=8.49 nM | SANGER | ||
| ETK-1 | Growth Inhibition Assay | IC50=7.88 nM | SANGER | ||
| LU-139 | Growth Inhibition Assay | IC50=7.77 nM | SANGER | ||
| KP-4 | Growth Inhibition Assay | IC50=7 nM | SANGER | ||
| HCC2218 | Growth Inhibition Assay | IC50=6.61 nM | SANGER | ||
| HN | Growth Inhibition Assay | IC50=5.96 nM | SANGER | ||
| AN3-CA | Growth Inhibition Assay | IC50=5.56 nM | SANGER | ||
| PC-3 | Growth Inhibition Assay | IC50=5.09 nM | SANGER | ||
| BPH-1 | Growth Inhibition Assay | IC50=4.76 nM | SANGER | ||
| BFTC-909 | Growth Inhibition Assay | IC50=3.71 nM | SANGER | ||
| NCI-H720 | Growth Inhibition Assay | IC50=3.57 nM | SANGER | ||
| MKN1 | Growth Inhibition Assay | IC50=2.8 nM | SANGER | ||
| SBC-1 | Growth Inhibition Assay | IC50=742 pM | SANGER | ||
| UM-UC-3 | Growth Inhibition Assay | IC50=315 pM | SANGER | ||
| PFSK-1 | Growth Inhibition Assay | IC50=49.06 nM | SANGER | ||
| 22RV1 | Growth Inhibition Assay | IC50=49.09 nM | SANGER | ||
| COR-L23 | Growth Inhibition Assay | IC50=49.16 nM | SANGER | ||
| D-283MED | Growth Inhibition Assay | IC50=49.61 nM | SANGER | ||
| SW982 | Growth Inhibition Assay | IC50=49.91 nM | SANGER | ||
| SW620 | Growth Inhibition Assay | IC50=50.36 nM | SANGER | ||
| KYSE-140 | Growth Inhibition Assay | IC50=50.55 nM | SANGER | ||
| GCIY | Growth Inhibition Assay | IC50=50.67 nM | SANGER | ||
| MHH-ESS-1 | Growth Inhibition Assay | IC50=51.95 nM | SANGER | ||
| D-423MG | Growth Inhibition Assay | IC50=52.08 nM | SANGER | ||
| SF539 | Growth Inhibition Assay | IC50=52.35 nM | SANGER | ||
| RPMI-2650 | Growth Inhibition Assay | IC50=52.69 nM | SANGER | ||
| GR-ST | Growth Inhibition Assay | IC50=52.87 nM | SANGER | ||
| YKG-1 | Growth Inhibition Assay | IC50=53 nM | SANGER | ||
| SK-MES-1 | Growth Inhibition Assay | IC50=53.26 nM | SANGER | ||
| HLE | Growth Inhibition Assay | IC50=53.47 nM | SANGER | ||
| RVH-421 | Growth Inhibition Assay | IC50=53.67 nM | SANGER | ||
| C32 | Growth Inhibition Assay | IC50=53.83 nM | SANGER | ||
| GB-1 | Growth Inhibition Assay | IC50=54.2 nM | SANGER | ||
| SNB75 | Growth Inhibition Assay | IC50=54.26 nM | SANGER | ||
| EM-2 | Growth Inhibition Assay | IC50=54.4 nM | SANGER | ||
| RH-1 | Growth Inhibition Assay | IC50=54.7 nM | SANGER | ||
| NKM-1 | Growth Inhibition Assay | IC50=54.81 nM | SANGER | ||
| NCI-H2405 | Growth Inhibition Assay | IC50=54.88 nM | SANGER | ||
| KYSE-450 | Growth Inhibition Assay | IC50=55.16 nM | SANGER | ||
| A704 | Growth Inhibition Assay | IC50=55.59 nM | SANGER | ||
| HAL-01 | Growth Inhibition Assay | IC50=55.83 nM | SANGER | ||
| TE-11 | Growth Inhibition Assay | IC50=55.99 nM | SANGER | ||
| DOK | Growth Inhibition Assay | IC50=56.02 nM | SANGER | ||
| KY821 | Growth Inhibition Assay | IC50=56.2 nM | SANGER | ||
| KGN | Growth Inhibition Assay | IC50=56.32 nM | SANGER | ||
| MC116 | Growth Inhibition Assay | IC50=57.8 nM | SANGER | ||
| PANC-08-13 | Growth Inhibition Assay | IC50=58.01 nM | SANGER | ||
| KE-37 | Growth Inhibition Assay | IC50=58.77 nM | SANGER | ||
| KYSE-410 | Growth Inhibition Assay | IC50=59.47 nM | SANGER | ||
| RO82-W-1 | Growth Inhibition Assay | IC50=59.9 nM | SANGER | ||
| M14 | Growth Inhibition Assay | IC50=60.04 nM | SANGER | ||
| GI-1 | Growth Inhibition Assay | IC50=60.3 nM | SANGER | ||
| ML-2 | Growth Inhibition Assay | IC50=60.62 nM | SANGER | ||
| BFTC-905 | Growth Inhibition Assay | IC50=60.65 nM | SANGER | ||
| DMS-273 | Growth Inhibition Assay | IC50=60.87 nM | SANGER | ||
| MDA-MB-361 | Growth Inhibition Assay | IC50=61 nM | SANGER | ||
| MSTO-211H | Growth Inhibition Assay | IC50=63.51 nM | SANGER | ||
| MEG-01 | Growth Inhibition Assay | IC50=63.52 nM | SANGER | ||
| M059J | Growth Inhibition Assay | IC50=63.58 nM | SANGER | ||
| LN-405 | Growth Inhibition Assay | IC50=63.85 nM | SANGER | ||
| NCI-H1581 | Growth Inhibition Assay | IC50=64.03 nM | SANGER | ||
| TCCSUP | Growth Inhibition Assay | IC50=64.53 nM | SANGER | ||
| SW872 | Growth Inhibition Assay | IC50=64.57 nM | SANGER | ||
| KYSE-510 | Growth Inhibition Assay | IC50=65.75 nM | SANGER | ||
| NCI-H1792 | Growth Inhibition Assay | IC50=66.15 nM | SANGER | ||
| SW13 | Growth Inhibition Assay | IC50=66.5 nM | SANGER | ||
| TE-8 | Growth Inhibition Assay | IC50=66.52 nM | SANGER | ||
| SCH | Growth Inhibition Assay | IC50=67.1 nM | SANGER | ||
| NEC8 | Growth Inhibition Assay | IC50=67.24 nM | SANGER | ||
| HuO-3N1 | Growth Inhibition Assay | IC50=67.31 nM | SANGER | ||
| EFM-19 | Growth Inhibition Assay | IC50=67.5 nM | SANGER | ||
| HEC-1 | Growth Inhibition Assay | IC50=67.52 nM | SANGER | ||
| T47D | Growth Inhibition Assay | IC50=67.87 nM | SANGER | ||
| SNU-423 | Growth Inhibition Assay | IC50=67.98 nM | SANGER | ||
| WM-115 | Growth Inhibition Assay | IC50=68.14 nM | SANGER | ||
| CaR-1 | Growth Inhibition Assay | IC50=68.25 nM | SANGER | ||
| KU812 | Growth Inhibition Assay | IC50=68.69 nM | SANGER | ||
| AM-38 | Growth Inhibition Assay | IC50=69.31 nM | SANGER | ||
| KOSC-2 | Growth Inhibition Assay | IC50=69.97 nM | SANGER | ||
| MC-IXC | Growth Inhibition Assay | IC50=70.08 nM | SANGER | ||
| SCC-4 | Growth Inhibition Assay | IC50=71.38 nM | SANGER | ||
| Calu-3 | Growth Inhibition Assay | IC50=71.98 nM | SANGER | ||
| RPMI-8866 | Growth Inhibition Assay | IC50=72.82 nM | SANGER | ||
| OVCAR-4 | Growth Inhibition Assay | IC50=73.36 nM | SANGER | ||
| OAW-42 | Growth Inhibition Assay | IC50=73.39 nM | SANGER | ||
| ATN-1 | Growth Inhibition Assay | IC50=73.87 nM | SANGER | ||
| CHP-212 | Growth Inhibition Assay | IC50=74.95 nM | SANGER | ||
| C2BBe1 | Growth Inhibition Assay | IC50=75.03 nM | SANGER | ||
| A498 | Growth Inhibition Assay | IC50=75.15 nM | SANGER | ||
| SH-4 | Growth Inhibition Assay | IC50=75.21 nM | SANGER | ||
| SNU-449 | Growth Inhibition Assay | IC50=75.79 nM | SANGER | ||
| RD | Growth Inhibition Assay | IC50=75.86 nM | SANGER | ||
| PANC-03-27 | Growth Inhibition Assay | IC50=76.25 nM | SANGER | ||
| S-117 | Growth Inhibition Assay | IC50=76.27 nM | SANGER | ||
| SK-MEL-2 | Growth Inhibition Assay | IC50=76.75 nM | SANGER | ||
| LK-2 | Growth Inhibition Assay | IC50=77.05 nM | SANGER | ||
| CP50-MEL-B | Growth Inhibition Assay | IC50=77.4 nM | SANGER | ||
| 647-V | Growth Inhibition Assay | IC50=78.07 nM | SANGER | ||
| LU-134-A | Growth Inhibition Assay | IC50=79.03 nM | SANGER | ||
| 5637 | Growth Inhibition Assay | IC50=79.23 nM | SANGER | ||
| NCI-H1437 | Growth Inhibition Assay | IC50=80.5 nM | SANGER | ||
| NCI-H460 | Growth Inhibition Assay | IC50=81.23 nM | SANGER | ||
| BxPC-3 | Growth Inhibition Assay | IC50=81.46 nM | SANGER | ||
| CAN | Growth Inhibition Assay | IC50=81.84 nM | SANGER | ||
| KINGS-1 | Growth Inhibition Assay | IC50=82.32 nM | SANGER | ||
| OCUB-M | Growth Inhibition Assay | IC50=82.41 nM | SANGER | ||
| KALS-1 | Growth Inhibition Assay | IC50=82.54 nM | SANGER | ||
| OCI-AML2 | Growth Inhibition Assay | IC50=82.61 nM | SANGER | ||
| A253 | Growth Inhibition Assay | IC50=82.65 nM | SANGER | ||
| LCLC-97TM1 | Growth Inhibition Assay | IC50=82.86 nM | SANGER | ||
| NCI-H520 | Growth Inhibition Assay | IC50=83.06 nM | SANGER | ||
| P30-OHK | Growth Inhibition Assay | IC50=83.5 nM | SANGER | ||
| SBC-5 | Growth Inhibition Assay | IC50=83.52 nM | SANGER | ||
| HCE-T | Growth Inhibition Assay | IC50=83.74 nM | SANGER | ||
| JEG-3 | Growth Inhibition Assay | IC50=84.1 nM | SANGER | ||
| KG-1 | Growth Inhibition Assay | IC50=84.24 nM | SANGER | ||
| MIA-PaCa-2 | Growth Inhibition Assay | IC50=84.54 nM | SANGER | ||
| CAL-33 | Growth Inhibition Assay | IC50=85.08 nM | SANGER | ||
| 639-V | Growth Inhibition Assay | IC50=85.42 nM | SANGER | ||
| NCI-H1048 | Growth Inhibition Assay | IC50=86.31 nM | SANGER | ||
| NCI-H1573 | Growth Inhibition Assay | IC50=87.48 nM | SANGER | ||
| NCI-H2228 | Growth Inhibition Assay | IC50=88.26 nM | SANGER | ||
| NB14 | Growth Inhibition Assay | IC50=88.3 nM | SANGER | ||
| SCC-25 | Growth Inhibition Assay | IC50=89.82 nM | SANGER | ||
| A431 | Growth Inhibition Assay | IC50=89.97 nM | SANGER | ||
| SN12C | Growth Inhibition Assay | IC50=90.62 nM | SANGER | ||
| HuCCT1 | Growth Inhibition Assay | IC50=90.76 nM | SANGER | ||
| LS-123 | Growth Inhibition Assay | IC50=92.18 nM | SANGER | ||
| CAL-85-1 | Growth Inhibition Assay | IC50=92.48 nM | SANGER | ||
| ES6 | Growth Inhibition Assay | IC50=92.83 nM | SANGER | ||
| NCI-H650 | Growth Inhibition Assay | IC50=94.09 nM | SANGER | ||
| NCI-H446 | Growth Inhibition Assay | IC50=95.12 nM | SANGER | ||
| EW-13 | Growth Inhibition Assay | IC50=95.75 nM | SANGER | ||
| HSC-2 | Growth Inhibition Assay | IC50=95.89 nM | SANGER | ||
| U031 | Growth Inhibition Assay | IC50=96.73 nM | SANGER | ||
| EW-11 | Growth Inhibition Assay | IC50=96.88 nM | SANGER | ||
| GAK | Growth Inhibition Assay | IC50=98.93 nM | SANGER | ||
| SK-OV-3 | Growth Inhibition Assay | IC50=100.07 nM | SANGER | ||
| OMC-1 | Growth Inhibition Assay | IC50=100.18 nM | SANGER | ||
| TK10 | Growth Inhibition Assay | IC50=100.21 nM | SANGER | ||
| EKVX | Growth Inhibition Assay | IC50=100.6 nM | SANGER | ||
| Detroit562 | Growth Inhibition Assay | IC50=102.17 nM | SANGER | ||
| SF268 | Growth Inhibition Assay | IC50=102.34 nM | SANGER | ||
| SNU-387 | Growth Inhibition Assay | IC50=104.17 nM | SANGER | ||
| MDA-MB-231 | Growth Inhibition Assay | IC50=105.06 nM | SANGER | ||
| NCI-H1563 | Growth Inhibition Assay | IC50=105.18 nM | SANGER | ||
| D-502MG | Growth Inhibition Assay | IC50=105.7 nM | SANGER | ||
| A2780 | Growth Inhibition Assay | IC50=106.47 nM | SANGER | ||
| IA-LM | Growth Inhibition Assay | IC50=107.51 nM | SANGER | ||
| D-392MG | Growth Inhibition Assay | IC50=107.54 nM | SANGER | ||
| MS-1 | Growth Inhibition Assay | IC50=107.71 nM | SANGER | ||
| SW1990 | Growth Inhibition Assay | IC50=108.54 nM | SANGER | ||
| HEL | Growth Inhibition Assay | IC50=109.29 nM | SANGER | ||
| SW1573 | Growth Inhibition Assay | IC50=109.31 nM | SANGER | ||
| SW1783 | Growth Inhibition Assay | IC50=110.22 nM | SANGER | ||
| COLO-680N | Growth Inhibition Assay | IC50=110.76 nM | SANGER | ||
| NCI-N87 | Growth Inhibition Assay | IC50=111.04 nM | SANGER | ||
| SK-MEL-28 | Growth Inhibition Assay | IC50=111.55 nM | SANGER | ||
| BT-20 | Growth Inhibition Assay | IC50=112.01 nM | SANGER | ||
| NCI-H1648 | Growth Inhibition Assay | IC50=113 nM | SANGER | ||
| no-11 | Growth Inhibition Assay | IC50=113.28 nM | SANGER | ||
| MOLT-13 | Growth Inhibition Assay | IC50=113.44 nM | SANGER | ||
| NCI-H2170 | Growth Inhibition Assay | IC50=114.51 nM | SANGER | ||
| HTC-C3 | Growth Inhibition Assay | IC50=116.85 nM | SANGER | ||
| LU-99A | Growth Inhibition Assay | IC50=117.21 nM | SANGER | ||
| HCC2998 | Growth Inhibition Assay | IC50=117.92 nM | SANGER | ||
| NB13 | Growth Inhibition Assay | IC50=117.99 nM | SANGER | ||
| GT3TKB | Growth Inhibition Assay | IC50=118.08 nM | SANGER | ||
| BT-549 | Growth Inhibition Assay | IC50=118.95 nM | SANGER | ||
| NCI-H747 | Growth Inhibition Assay | IC50=119.34 nM | SANGER | ||
| EW-1 | Growth Inhibition Assay | IC50=120.2 nM | SANGER | ||
| LB831-BLC | Growth Inhibition Assay | IC50=120.63 nM | SANGER | ||
| NMC-G1 | Growth Inhibition Assay | IC50=121.11 nM | SANGER | ||
| COLO-679 | Growth Inhibition Assay | IC50=122.15 nM | SANGER | ||
| HL-60 | Growth Inhibition Assay | IC50=123.1 nM | SANGER | ||
| MKN7 | Growth Inhibition Assay | IC50=123.83 nM | SANGER | ||
| RERF-LC-MS | Growth Inhibition Assay | IC50=124.31 nM | SANGER | ||
| DMS-114 | Growth Inhibition Assay | IC50=125.09 nM | SANGER | ||
| HuP-T4 | Growth Inhibition Assay | IC50=126.97 nM | SANGER | ||
| HCC2157 | Growth Inhibition Assay | IC50=127.5 nM | SANGER | ||
| SKG-IIIa | Growth Inhibition Assay | IC50=128.8 nM | SANGER | ||
| HCT-116 | Growth Inhibition Assay | IC50=130.64 nM | SANGER | ||
| BB30-HNC | Growth Inhibition Assay | IC50=130.78 nM | SANGER | ||
| KYSE-270 | Growth Inhibition Assay | IC50=130.88 nM | SANGER | ||
| MFM-223 | Growth Inhibition Assay | IC50=131.51 nM | SANGER | ||
| NH-12 | Growth Inhibition Assay | IC50=132.99 nM | SANGER | ||
| U-118-MG | Growth Inhibition Assay | IC50=133.62 nM | SANGER | ||
| ESS-1 | Growth Inhibition Assay | IC50=135.18 nM | SANGER | ||
| D-247MG | Growth Inhibition Assay | IC50=135.21 nM | SANGER | ||
| IGROV-1 | Growth Inhibition Assay | IC50=135.76 nM | SANGER | ||
| C-33-A | Growth Inhibition Assay | IC50=135.97 nM | SANGER | ||
| NCI-H1693 | Growth Inhibition Assay | IC50=136.12 nM | SANGER | ||
| MLMA | Growth Inhibition Assay | IC50=136.58 nM | SANGER | ||
| SK-N-AS | Growth Inhibition Assay | IC50=137.17 nM | SANGER | ||
| NCI-H1755 | Growth Inhibition Assay | IC50=138.85 nM | SANGER | ||
| CHP-134 | Growth Inhibition Assay | IC50=139.55 nM | SANGER | ||
| LS-513 | Growth Inhibition Assay | IC50=140.91 pM | SANGER | ||
| TE-12 | Growth Inhibition Assay | IC50=140.93 nM | SANGER | ||
| KNS-42 | Growth Inhibition Assay | IC50=144.3 nM | SANGER | ||
| SJRH30 | Growth Inhibition Assay | IC50=144.44 nM | SANGER | ||
| NCI-H1092 | Growth Inhibition Assay | IC50=144.52 nM | SANGER | ||
| H-EMC-SS | Growth Inhibition Assay | IC50=146.81 nM | SANGER | ||
| SK-MEL-3 | Growth Inhibition Assay | IC50=147.55 nM | SANGER | ||
| SK-N-FI | Growth Inhibition Assay | IC50=147.59 nM | SANGER | ||
| NCI-H2126 | Growth Inhibition Assay | IC50=148.15 nM | SANGER | ||
| NCI-H1299 | Growth Inhibition Assay | IC50=150.22 nM | SANGER | ||
| CFPAC-1 | Growth Inhibition Assay | IC50=150.66 nM | SANGER | ||
| NCI-H661 | Growth Inhibition Assay | IC50=151.26 nM | SANGER | ||
| KYSE-70 | Growth Inhibition Assay | IC50=151.79 nM | SANGER | ||
| SW900 | Growth Inhibition Assay | IC50=154.65 nM | SANGER | ||
| Ca-Ski | Growth Inhibition Assay | IC50=156.39 nM | SANGER | ||
| HPAF-II | Growth Inhibition Assay | IC50=156.47 nM | SANGER | ||
| LB2518-MEL | Growth Inhibition Assay | IC50=157.1 nM | SANGER | ||
| LC-2-ad | Growth Inhibition Assay | IC50=158.62 nM | SANGER | ||
| HCC1806 | Growth Inhibition Assay | IC50=167.88 nM | SANGER | ||
| UACC-62 | Growth Inhibition Assay | IC50=168.09 nM | SANGER | ||
| KM-H2 | Growth Inhibition Assay | IC50=170.58 nM | SANGER | ||
| NCI-H2347 | Growth Inhibition Assay | IC50=172.72 nM | SANGER | ||
| SCC-15 | Growth Inhibition Assay | IC50=173.66 nM | SANGER | ||
| BB49-HNC | Growth Inhibition Assay | IC50=173.81 nM | SANGER | ||
| GMS-10 | Growth Inhibition Assay | IC50=173.94 nM | SANGER | ||
| NCI-H2052 | Growth Inhibition Assay | IC50=174.9 nM | SANGER | ||
| SW626 | Growth Inhibition Assay | IC50=176.06 nM | SANGER | ||
| MDA-MB-415 | Growth Inhibition Assay | IC50=176.61 nM | SANGER | ||
| Saos-2 | Growth Inhibition Assay | IC50=179.35 nM | SANGER | ||
| DK-MG | Growth Inhibition Assay | IC50=180.3 nM | SANGER | ||
| SNU-C2B | Growth Inhibition Assay | IC50=180.73 nM | SANGER | ||
| A427 | Growth Inhibition Assay | IC50=182.57 nM | SANGER | ||
| KP-N-YS | Growth Inhibition Assay | IC50=185 nM | SANGER | ||
| J82 | Growth Inhibition Assay | IC50=185.18 nM | SANGER | ||
| LS-411N | Growth Inhibition Assay | IC50=187.28 nM | SANGER | ||
| HCC1937 | Growth Inhibition Assay | IC50=187.49 nM | SANGER | ||
| OE33 | Growth Inhibition Assay | IC50=188.97 nM | SANGER | ||
| NB7 | Growth Inhibition Assay | IC50=189.89 nM | SANGER | ||
| SW684 | Growth Inhibition Assay | IC50=196.13 nM | SANGER | ||
| HT-144 | Growth Inhibition Assay | IC50=196.15 nM | SANGER | ||
| SK-MEL-30 | Growth Inhibition Assay | IC50=196.2 nM | SANGER | ||
| DBTRG-05MG | Growth Inhibition Assay | IC50=198.47 nM | SANGER | ||
| NCI-H1395 | Growth Inhibition Assay | IC50=198.85 nM | SANGER | ||
| NCI-H2122 | Growth Inhibition Assay | IC50=200.59 nM | SANGER | ||
| no-10 | Growth Inhibition Assay | IC50=201.04 nM | SANGER | ||
| SW48 | Growth Inhibition Assay | IC50=201.31 nM | SANGER | ||
| NCI-H1650 | Growth Inhibition Assay | IC50=204.01 nM | SANGER | ||
| MZ1-PC | Growth Inhibition Assay | IC50=205.58 nM | SANGER | ||
| U-266 | Growth Inhibition Assay | IC50=205.79 nM | SANGER | ||
| CAS-1 | Growth Inhibition Assay | IC50=207.44 nM | SANGER | ||
| AU565 | Growth Inhibition Assay | IC50=212.82 nM | SANGER | ||
| UACC-257 | Growth Inhibition Assay | IC50=213.99 nM | SANGER | ||
| CAL-27 | Growth Inhibition Assay | IC50=217.05 nM | SANGER | ||
| NCI-H23 | Growth Inhibition Assay | IC50=219.33 nM | SANGER | ||
| TE-6 | Growth Inhibition Assay | IC50=219.68 nM | SANGER | ||
| TGBC24TKB | Growth Inhibition Assay | IC50=222.17 nM | SANGER | ||
| TE-1 | Growth Inhibition Assay | IC50=222.88 nM | SANGER | ||
| RCC10RGB | Growth Inhibition Assay | IC50=224.19 nM | SANGER | ||
| NCI-H596 | Growth Inhibition Assay | IC50=228.22 nM | SANGER | ||
| SW954 | Growth Inhibition Assay | IC50=233.83 nM | SANGER | ||
| NCI-H2087 | Growth Inhibition Assay | IC50=234.51 nM | SANGER | ||
| SK-PN-DW | Growth Inhibition Assay | IC50=235.19 nM | SANGER | ||
| KM12 | Growth Inhibition Assay | IC50=235.7 nM | SANGER | ||
| BT-474 | Growth Inhibition Assay | IC50=235.73 nM | SANGER | ||
| IST-MES1 | Growth Inhibition Assay | IC50=236.57 nM | SANGER | ||
| HT-1197 | Growth Inhibition Assay | IC50=238.09 nM | SANGER | ||
| CAL-54 | Growth Inhibition Assay | IC50=238.49 nM | SANGER | ||
| NB10 | Growth Inhibition Assay | IC50=240.06 nM | SANGER | ||
| PANC-10-05 | Growth Inhibition Assay | IC50=245.56 nM | SANGER | ||
| NCI-H522 | Growth Inhibition Assay | IC50=248.31 nM | SANGER | ||
| A388 | Growth Inhibition Assay | IC50=249.82 nM | SANGER | ||
| GOTO | Growth Inhibition Assay | IC50=250.29 nM | SANGER | ||
| KLE | Growth Inhibition Assay | IC50=251.87 nM | SANGER | ||
| KYSE-520 | Growth Inhibition Assay | IC50=252.86 nM | SANGER | ||
| HCE-4 | Growth Inhibition Assay | IC50=262.5 nM | SANGER | ||
| KURAMOCHI | Growth Inhibition Assay | IC50=265.9 nM | SANGER | ||
| HCC38 | Growth Inhibition Assay | IC50=266.48 nM | SANGER | ||
| FADU | Growth Inhibition Assay | IC50=266.63 nM | SANGER | ||
| CW-2 | Growth Inhibition Assay | IC50=269.96 nM | SANGER | ||
| L-428 | Growth Inhibition Assay | IC50=275.15 nM | SANGER | ||
| HCC1569 | Growth Inhibition Assay | IC50=275.84 nM | SANGER | ||
| NCI-H810 | Growth Inhibition Assay | IC50=278.31 nM | SANGER | ||
| LB771-HNC | Growth Inhibition Assay | IC50=285.84 nM | SANGER | ||
| LCLC-103H | Growth Inhibition Assay | IC50=285.99 nM | SANGER | ||
| EFO-21 | Growth Inhibition Assay | IC50=287.68 nM | SANGER | ||
| CAL-72 | Growth Inhibition Assay | IC50=293.19 nM | SANGER | ||
| SCC-9 | Growth Inhibition Assay | IC50=293.22 nM | SANGER | ||
| COLO-829 | Growth Inhibition Assay | IC50=296.5 nM | SANGER | ||
| U-87-MG | Growth Inhibition Assay | IC50=300.73 nM | SANGER | ||
| MZ7-mel | Growth Inhibition Assay | IC50=323.76 nM | SANGER | ||
| NCI-H1770 | Growth Inhibition Assay | IC50=326.74 nM | SANGER | ||
| ChaGo-K-1 | Growth Inhibition Assay | IC50=328.1 nM | SANGER | ||
| SiHa | Growth Inhibition Assay | IC50=329.24 nM | SANGER | ||
| NCI-SNU-5 | Growth Inhibition Assay | IC50=336.77 nM | SANGER | ||
| DJM-1 | Growth Inhibition Assay | IC50=340.33 nM | SANGER | ||
| OE19 | Growth Inhibition Assay | IC50=340.53 nM | SANGER | ||
| NCI-H1651 | Growth Inhibition Assay | IC50=344.18 nM | SANGER | ||
| COLO-792 | Growth Inhibition Assay | IC50=354.42 nM | SANGER | ||
| ACHN | Growth Inhibition Assay | IC50=356.71 nM | SANGER | ||
| TH-3 | Growth Inhibition Assay | IC50=379.95 nM | SANGER | ||
| HT-1376 | Growth Inhibition Assay | IC50=384.88 nM | SANGER | ||
| RH-18 | Growth Inhibition Assay | IC50=394.74 nM | SANGER | ||
| NB6 | Growth Inhibition Assay | IC50=396.66 nM | SANGER | ||
| COLO-320-HSR | Growth Inhibition Assay | IC50=403.37 nM | SANGER | ||
| UACC-893 | Growth Inhibition Assay | IC50=406.47 nM | SANGER | ||
| DSH1 | Growth Inhibition Assay | IC50=406.91 nM | SANGER | ||
| TE-10 | Growth Inhibition Assay | IC50=407.01 nM | SANGER | ||
| HCC70 | Growth Inhibition Assay | IC50=409.21 nM | SANGER | ||
| TGBC11TKB | Growth Inhibition Assay | IC50=410.33 nM | SANGER | ||
| NCI-H727 | Growth Inhibition Assay | IC50=412.11 nM | SANGER | ||
| ALL-PO | Growth Inhibition Assay | IC50=415.69 nM | SANGER | ||
| ABC-1 | Growth Inhibition Assay | IC50=420.45 nM | SANGER | ||
| NCI-H69 | Growth Inhibition Assay | IC50=426.76 nM | SANGER | ||
| GP5d | Growth Inhibition Assay | IC50=434.41 nM | SANGER | ||
| UMC-11 | Growth Inhibition Assay | IC50=458.36 nM | SANGER | ||
| RMG-I | Growth Inhibition Assay | IC50=467.56 nM | SANGER | ||
| YAPC | Growth Inhibition Assay | IC50=490.6 nM | SANGER | ||
| LS-1034 | Growth Inhibition Assay | IC50=491.06 nM | SANGER | ||
| RCM-1 | Growth Inhibition Assay | IC50=496.68 nM | SANGER | ||
| HCC1954 | Growth Inhibition Assay | IC50=512.5 nM | SANGER | ||
| SK-MEL-24 | Growth Inhibition Assay | IC50=516.51 nM | SANGER | ||
| NB12 | Growth Inhibition Assay | IC50=528.42 nM | SANGER | ||
| SW756 | Growth Inhibition Assay | IC50=554.96 nM | SANGER | ||
| HCC1187 | Growth Inhibition Assay | IC50=575.83 nM | SANGER | ||
| NCI-H2342 | Growth Inhibition Assay | IC50=590.39 nM | SANGER | ||
| NCI-H2291 | Growth Inhibition Assay | IC50=598.31 nM | SANGER | ||
| OVCAR-3 | Growth Inhibition Assay | IC50=598.96 nM | SANGER | ||
| MHH-NB-11 | Growth Inhibition Assay | IC50=629.01 nM | SANGER | ||
| SAS | Growth Inhibition Assay | IC50=652.67 nM | SANGER | ||
| COLO-824 | Growth Inhibition Assay | IC50=689.37 nM | SANGER | ||
| HCC1395 | Growth Inhibition Assay | IC50=698.5 nM | SANGER | ||
| COLO-668 | Growth Inhibition Assay | IC50=706.1 nM | SANGER | ||
| NCI-H226 | Growth Inhibition Assay | IC50=707.8 nM | SANGER | ||
| NB17 | Growth Inhibition Assay | IC50=721.75 nM | SANGER | ||
| SW1463 | Growth Inhibition Assay | IC50=739.19 nM | SANGER | ||
| TGW | Growth Inhibition Assay | IC50=760.15 nM | SANGER | ||
| NCI-H526 | Growth Inhibition Assay | IC50=823.53 nM | SANGER | ||
| COR-L88 | Growth Inhibition Assay | IC50=848.12 nM | SANGER | ||
| NCI-H441 | Growth Inhibition Assay | IC50=895.22 nM | SANGER | ||
| NCI-H630 | Growth Inhibition Assay | IC50=912.96 nM | SANGER | ||
| Mo-T | Growth Inhibition Assay | IC50=947.88 nM | SANGER | ||
| JAR | Growth Inhibition Assay | IC50=956.24 nM | SANGER | ||
| NCI-H1838 | Growth Inhibition Assay | IC50=1.02388 μM | SANGER | ||
| DoTc2-4510 | Growth Inhibition Assay | IC50=1.07376 μM | SANGER | ||
| MKN28 | Growth Inhibition Assay | IC50=1.09024 μM | SANGER | ||
| HuP-T3 | Growth Inhibition Assay | IC50=1.11905 μM | SANGER | ||
| TE-9 | Growth Inhibition Assay | IC50=1.12973 μM | SANGER | ||
| NY | Growth Inhibition Assay | IC50=1.16792 μM | SANGER | ||
| HT55 | Growth Inhibition Assay | IC50=1.31344 μM | SANGER | ||
| SW837 | Growth Inhibition Assay | IC50=1.32978 μM | SANGER | ||
| NCI-H2029 | Growth Inhibition Assay | IC50=1.41791 μM | SANGER | ||
| IST-SL1 | Growth Inhibition Assay | IC50=1.4424 μM | SANGER | ||
| COLO-741 | Growth Inhibition Assay | IC50=1.49771 μM | SANGER | ||
| LU-65 | Growth Inhibition Assay | IC50=1.62249 μM | SANGER | ||
| NCI-H1304 | Growth Inhibition Assay | IC50=1.65498 μM | SANGER | ||
| KARPAS-299 | Growth Inhibition Assay | IC50=1.79479 μM | SANGER | ||
| NCI-H358 | Growth Inhibition Assay | IC50=1.95503 μM | SANGER | ||
| OAW-28 | Growth Inhibition Assay | IC50=2.06919 μM | SANGER | ||
| C8166 | Growth Inhibition Assay | IC50=2.63392 μM | SANGER | ||
| COLO-678 | Growth Inhibition Assay | IC50=2.83768 μM | SANGER | ||
| SK-N-DZ | Growth Inhibition Assay | IC50=2.86381 μM | SANGER | ||
| NCI-H82 | Growth Inhibition Assay | IC50=2.90369 μM | SANGER | ||
| JVM-2 | Growth Inhibition Assay | IC50=3.03188 μM | SANGER | ||
| SW1116 | Growth Inhibition Assay | IC50=3.05411 μM | SANGER | ||
| MDA-MB-453 | Growth Inhibition Assay | IC50=3.10439 μM | SANGER | ||
| Calu-6 | Growth Inhibition Assay | IC50=3.1997 μM | SANGER | ||
| SHP-77 | Growth Inhibition Assay | IC50=3.528 μM | SANGER | ||
| Capan-2 | Growth Inhibition Assay | IC50=4.32581 μM | SANGER | ||
| SW948 | Growth Inhibition Assay | IC50=4.74779 μM | SANGER | ||
| HDLM-2 | Growth Inhibition Assay | IC50=5.07725 μM | SANGER | ||
| LAN-6 | Growth Inhibition Assay | IC50=6.21495 μM | SANGER | ||
| LU-135 | Growth Inhibition Assay | IC50=6.43077 μM | SANGER | ||
| T84 | Growth Inhibition Assay | IC50=6.9864 μM | SANGER | ||
| CAPAN-1 | Growth Inhibition Assay | IC50=7.62233 μM | SANGER | ||
| SW1417 | Growth Inhibition Assay | IC50=7.91731 μM | SANGER | ||
| BALL-1 | Growth Inhibition Assay | IC50=8.50409 μM | SANGER | ||
| HT-29 | Growth Inhibition Assay | IC50=9.07599 μM | SANGER | ||
| C3A | Growth Inhibition Assay | IC50=9.88394 μM | SANGER | ||
| NCI-H1993 | Growth Inhibition Assay | IC50=10.5081 μM | SANGER | ||
| SK-MEL-1 | Growth Inhibition Assay | IC50=11.6289 μM | SANGER | ||
| DU-145 | Growth Inhibition Assay | IC50=14.5052 μM | SANGER | ||
| KP-N-YN | Growth Inhibition Assay | IC50=14.5103 μM | SANGER | ||
| CCRF-CEM | Growth Inhibition Assay | IC50=14.7809 μM | SANGER | ||
| ZR-75-30 | Growth Inhibition Assay | IC50=16.3303 μM | SANGER | ||
| A673 | Growth Inhibition Assay | IC50=20.5507 μM | SANGER | ||
| K-562 | Growth Inhibition Assay | IC50=28.4183 μM | SANGER | ||
| 点击查看更多细胞系数据 | |||||
生物活性
| 产品描述 | Dactolisib (BEZ235, NVP-BEZ235) 是一种双重ATP竞争性 PI3K 和 mTOR 抑制剂，在无细胞试验中，抑制 p110α/γ/δ/β 和 mTOR(p70S6K) 的 IC50 分别为 4 nM /5 nM /7 nM /75 nM /6 nM。 在 3T3TopBP1-ER 细胞中抑制 ATR，IC50 为 21 nM，而对 Akt 和 PDK1 的抑制作用很弱。Dactolisib可诱导自噬并抑制HIV-1的复制。Phase 2。 | |||||||||||
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| 靶点 |
|
| 体外研究(In Vitro) | ||||
| 体外研究活性 | BEZ235显著降低mTOR活化的激酶p70S6K的磷酸化水平。BEZ235导致S235/S236P-RPS6水平减少，IC50为6.5 nM。BEZ235抗mTOR的活性使用生化mTOR K-LISA试验测定，IC50为20.7 nM。BEZ235对其β旁系同源物的活性稍弱，IC50为75 nM。在人肿瘤细胞中，PI3K/Akt/mTOR通路经常被组成性活化。BEZ235阻断PI3K和mTOR激酶活性，通过结合于这些酶的ATP结合槽发挥作用。用逐渐增加浓度BEZ235处理PTEN-null细胞系PC3M和U87MG时，导致细胞增殖剂量依赖性减少，平均GI50为10-12 nM。[1] BEZ235是一种mTORC1/2催化抑制剂。[2] | |||
|---|---|---|---|---|
| 激酶实验 | 体外蛋白激酶,PI3K,和mTOR实验 | |||
| PI3Kα, β, δ蛋白都由与p110全长蛋白相接的p85 N端的iSH2域组成，只是PI3Kα没有最后的20个氨基酸。PI3Kγ由p110全长蛋白去掉前144个氨基酸产生而来。所有PI3K蛋白在羧基末端加组氨酸标签便于纯化，然后克隆到pBlue-Bac4.5 (用于α, β,和δ亚型) 或者pVL1393 (用于γ 亚型) 质粒中。转染BaculoGold WT基因组DNA的不同的载体按说明书推荐的方法生产各自重组体杆状病毒及重组蛋白。使用激酶发光检测试剂盒测定BEZ235 (NVP-BEZ235)作用于PI3K的活力。在384孔板上进行激酶实验。在每个孔中加入50 nl的测试项目（溶在90%DMSO中）和5ul的反应buffer,反应buffer包含10 μg/ml PI基质 (l-α-磷脂酰肌醇; 由Avanti Polar Lipids提供;预备在3%辛基葡萄糖苷中)，然后加入PI3K 蛋白(p110α, p110β, p110δ,和p110γ分别为10, 25, 10,和150 nM)。加入预备在反应buffer中的5 ul 1 µM 的ATP反应开始，反应进行60分钟 (测p110α, p110β, p110δ)或者120分钟(测p110γ)，随后加入10ul的荧光激酶buffer终止反应。数据用Synergy 2 阅读器阅读用于荧光测试。 | ||||
| 细胞实验 | 细胞系 | HCT116, DLD-1, SW480 | ||
| 浓度 | 0-1 μM | |||
| 孵育时间 | 48小时 | |||
| 方法 | HCT116 (PIK3CA突变型; 激酶域在H1047R), DLD-1 (PIK3CA突变型；螺旋域在E545K), SW480 (PIK3CA 野生型)人类CRC细胞系，同基因型的DLD-1 PIK3CA突变和野生型细胞培养在含10%FBS和1×青霉素/链霉素的培养基中。细胞按不同的初始密度加入（HCT116: 3000个细胞/每孔, DLD-1: 5500个细胞/每孔, SW480: 4500个细胞/每孔, DLD-1 PIK3CA突变型: 7000个细胞/每孔, DLD-1 PIK3CA野生型: 9000个细胞/每孔)，用来计算不同的生长动力学。16个小时后，细胞加入浓度越来越高的BEZ235中进行温育，含有药物的培养基24小时更换一次。根据产品说明书，加入细胞16小时和药物处理48小时，使用单溶液细胞增殖检测试剂盒以比色法检测细胞活力。与没有用药物处理正在生长的细胞相比，药物处理的细胞的活力也逐渐趋于正常化。使用GraphPad Prism 5软件用4个参数的回归曲线计算IC50值。用于western blot 分析，细胞用0 nM 或者最高抑制剂量(500 nM) BEZ235处理 2, 6, 24, 或者48 小时。 |
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| 实验图片 | 检测方法 | 检测指标 | 实验图片 | PMID |
| Western blot | Myc / Vinculin / pT58 Myc pAkt / Akt / Skp2 / AR / pS6 / p27 p-S6K / S6K / p-Akt / Akt / p-ABL / BCR-ABL Bcl-2 / Caspase-3 / Cleaved caspase-3 Cyclin D1 / Cyclin D2 mTOR / p-mTOR / p70S6K / p-p70S6K p-EGFR-Tyr1068 / EGFR / p-HER2-Tyr1221 / p-HER2-Tyr1222 / HER2 / p-HER3-Tyr1289 |
|
25934076 | |
| Immunofluorescence | SP1 p-ErbB2(Y1248) LC3 |
|
26336820 | |
| Growth inhibition assay | Cell viability (P3, U87) Cell viability (breast cancer cells) Cell viability (K562, KBM7R) |
|
27542970 | |
| ELISA | VEGF |
|
19671762 | |
| 体内研究(In Vivo) | ||
| 体内研究活性 | BEZ235诱导肿瘤(69%)消退，而对体重增加没有统计学上显著的作用。总之，这些初步的体内功效研究结果表明，BEZ235单一口服给药时能够阻断疾病的发展，与其他抗癌药结合使用时能够增强疗效。[1] | |
|---|---|---|
| 动物实验 | Animal Models | 雌性Harlan无胸腺裸鼠 |
| Dosages | 45 mg/kg | |
| Administration | 口服处理 | |
| NCT Number | Recruitment | Conditions | Sponsor/Collaborators | Start Date | Phases |
|---|---|---|---|---|---|
| NCT01856101 | Terminated | Carcinoma Transitional Cell |
Cliniques universitaires Saint-Luc- Université Catholique de Louvain|Novartis |
February 2013 | Phase 2 |
| NCT01717898 | Terminated | Castrate-resistant Prostate Cancer |
Charles Ryan|Novartis Pharmaceuticals|University of California San Francisco |
January 31 2013 | Phase 1|Phase 2 |
| NCT01756118 | Completed | Acute Lymphoblastic Leukemia|Leukemia Myelocytic Acute|Chronic Myelogenous Leukemia With Crisis of Blast Cells |
Goethe University |
June 2012 | Phase 1 |
| NCT01290406 | Withdrawn | Endometrial Cancer |
Novartis Pharmaceuticals|Novartis |
March 2012 | Phase 2 |
| NCT01288092 | Withdrawn | Metastatic Breast Cancer |
Novartis Pharmaceuticals|Novartis |
March 2012 | Phase 2 |
化学信息&溶解度
| 分子量 | 469.55 | 分子式 | C30H23N5O |
| CAS号 | 915019-65-7 | SDF | Download Dactolisib (BEZ235) SDF |
| Smiles | CC(C)(C#N)C1=CC=C(C=C1)N2C3=C4C=C(C=CC4=NC=C3N(C2=O)C)C5=CC6=CC=CC=C6N=C5 | ||
| 储存条件(自收到货起) | |||
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体外溶解度 |
DMSO : 9 mg/mL ( (19.16 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 |
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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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* 必填项
常见问题及建议解决方法
问题 1:
With difficulties in dissolving BEZ235, How can I improve its solubility?
回答：
For in vivo study, we suggest the vehicle solution NMP/polyethylene glycol 300 (10/90, v/v). Please dissolve BEZ235 in NMP as more as possible. You can sonicate and warm it in water bath for a while. Then dilute with PEG 300.
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