- 阻害剤
- 研究分野別
- PI3K/Akt/mTOR
- Epigenetics
- Methylation
- Immunology & Inflammation
- Protein Tyrosine Kinase
- Angiogenesis
- Apoptosis
- Autophagy
- ER stress & UPR
- JAK/STAT
- MAPK
- Cytoskeletal Signaling
- Cell Cycle
- TGF-beta/Smad
- 化合物ライブラリー
- 抗体
- 新製品
- お問い合わせ
Dactolisib (BEZ235)
別名：NVP-BEZ235
Dactolisib (BEZ235, NVP-BEZ235) is a dual ATP-competitive PI3K and mTOR inhibitor for p110α/γ/δ/β and mTOR(p70S6K) with IC50 of 4 nM /5 nM /7 nM /75 nM /6 nM in cell-free assays, respectively. Inhibits ATR with IC50 of 21 nM in 3T3TopBP1-ER cell. Dactolisib induces autophagy and suppresses HIV-1 replication. Phase 2.
CAS No. 915019-65-7
文献中Selleckの製品使用例（470）
製品安全説明書
現在のバッチを見る：
純度：
99.99%
99.99
Dactolisib (BEZ235)関連製品
| 関連ターゲット | p110α p110β p110δ p110γ C2β Vps34 | もっと見る |
|---|---|---|
| 関連化合物ライブラリー | Kinase Inhibitor Library PI3K/Akt Inhibitor Library Apoptosis Compound Library Cell Cycle compound library NF-κB Signaling Compound Library | もっと見る |
シグナル伝達経路
PI3K阻害剤の選択性比較
Cell Data
| Cell Lines | Assay Type | Concentration | Incubation Time | 活性情報 | PMID |
|---|---|---|---|---|---|
| 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 | ||
| 他の多くの細胞株試験データをご覧になる場合はこちらをクリックして下さい | |||||
生物活性
| 製品説明 | Dactolisib (BEZ235, NVP-BEZ235) is a dual ATP-competitive PI3K and mTOR inhibitor for p110α/γ/δ/β and mTOR(p70S6K) with IC50 of 4 nM /5 nM /7 nM /75 nM /6 nM in cell-free assays, respectively. Inhibits ATR with IC50 of 21 nM in 3T3TopBP1-ER cell. Dactolisib induces autophagy and suppresses HIV-1 replication. Phase 2. | |||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|
| Targets |
|
| In Vitro | ||||
| In vitro | BEZ235 significantly reduces the phosphorylation levels of the mTOR activated kinase p70S6K. BEZ235 results in a reduction of S235/S236P-RPS6 levels with IC50 of 6.5 nM. The activity of BEZ235 against mTOR is determined using a biochemical mTOR K-LISA assay with IC50 of 20.7 nM. BEZ235 shows slightly lower activity against its β paralogue with IC50 of 75 nM. The PI3K/Akt/mTOR pathway is often constitutively activated in human tumor cells. BEZ235 blocks PI3K and mTOR kinase activity by binding to the ATP-binding cleft of these enzymes. Both PTEN-null cell lines PC3M and U87MG show a dose-dependent reduction in cell proliferation when treated with increasing concentrations of BEZ235 with an average GI50 of 10-12 nM. [1] BEZ235 is an mTORC1/2 catalytic inhibitor. [2] | |||
|---|---|---|---|---|
| Kinase Assay | In vitro Protein Kinase, PI3K, and mTOR Assays | |||
| PI3Kα, β, and δ proteins are composed of the iSH2 domain of p85 NH2-terminally fused to the full-length protein p110 protein, with the exception of α that also does not contain the last 20 amino acids. PI3Kγ is produced as full-length protein deleted for its first 144 amino acids. All constructs are fused to a COOH-terminal His tag for convenient purification and then cloned into the pBlue-Bac4.5 (for α, β, and δ isoforms) or pVL1393 (for γ isoform) plasmids. The different vectors are then cotransfected with BaculoGold WT genomic DNA using methods recommended by the vendor for production of the respective recombinant baculoviruses and proteins. BEZ235 are tested for their activity against PI3K using a Kinase-Glo assay. The kinase reaction is done in 384-well black plate. Each well is loaded with 50 μL of test items (in 90% DMSO) and 5 μL reaction buffer containing 10 μg/mL PI substrate (l-α-phosphatidylinositol; Avanti Polar Lipids; prepared in 3% octyl-glucoside) and the PI3K proteins (10, 25, 10, and 150 nM of p110α, p110β, p110δ, and p110γ, respectively) are then added to it. The reaction is started by the addition of 5 μL of 1 μM ATP prepared in the reaction buffer and is incubated for either 60 (for p110α, p110β, and p110δ) or 120 min (for p110γ). It is terminated by the addition of 10 μL Kinase-Glo buffer. The plates are then read in a Synergy 2 reader for luminescence detection. | ||||
| 細胞実験 | 細胞株 | HCT116, DLD-1 and SW480 cells | ||
| 濃度 | 0-1 μM | |||
| 反応時間 | 48 hours | |||
| 実験の流れ | The human CRC cell lines, HCT116 (PIK3CA mutant; kinase domain at H1047R), DLD-1 (PIK3CA mutant; helical domain at E545K), and SW480 (PIK3CA wild-type) and isogenic DLD-1 PIK3CA mutant as well as wild-type cells are maintained in DMEM with 10% FBS and 1 × Penicillin/Streptomycin. Cells are plated at different initial densities (HCT116: 3 × 103 cells/well, DLD-1: 5.5 × 103 cells/well, SW480: 4.5 × 103 cells/well, DLD-1 PIK3CA mutant: 7 × 103 cells/well, and DLD-1 PIK3CA wild-type: 9 × 103 cells/well) to account for differential growth kinetics. After 16 hours, cells are incubated with increasing concentrations of BEZ235, and the drug-containing growth medium is changed every 24 hours. Cell viability is assessed 16 hours after the initial plating and 48 hours after initiation of drug treatment using the colorimetric MTS assay CellTiter 96® AQueous One Solution Cell Proliferation Assay, as per the manufacturer's instructions. Cell viability after drug treatment is normalized to that of untreated cells also grown for 48 hours. For western blot analysis, cells are plated with zero or maximum inhibitory dose (500 nM) BEZ235 for 2, 6, 24, or 48 hours. |
|||
| 実験結果図 | Methods | Biomarkers | 結果図 | 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 | |
| In Vivo | ||
| In Vivo | BEZ235 induces regression of the tumors (69%) without statistically significant effect on body weight gain. Altogether, these preliminary in vivo efficacy results show that BEZ235 causes disease stasis when administered orally as a single agent and can enhance the efficacy of other anticancer agents when used in combination studies. [1] | |
|---|---|---|
| 動物実験 | 動物モデル | Female Harlan athymic nude mice |
| 投与量 | 45 mg/kg | |
| 投与経路 | p.o. | |
| 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 |
化学情報
| 分子量 | 469.55 | 化学式 | C30H23N5O |
| CAS No. | 915019-65-7 | SDF | Download Dactolisib (BEZ235) SDFをダウンロードする |
| 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 | ||
| 保管 | |||
|
In vitro |
DMSO : 9 mg/mL ( (19.16 mM)； 吸湿したDMSOは溶解度を減少させます。新しいDMSOをご使用ください。) Water : Insoluble Ethanol : Insoluble |
モル濃度計算器 |
|
in vivo Add solvents to the product individually and in order. |
投与溶液組成計算機 | ||||
実験計算
投与溶液組成計算機(クリア溶液)
ステップ１：実験データを入力してください。（実験操作によるロスを考慮し、動物数を1匹分多くして計算・調製することを推奨します）
mg/kg
g
μL
匹
ステップ２：投与溶媒の組成を入力してください。（ロット毎に適した溶解組成が異なる場合があります。詳細については弊社までお問い合わせください）
% DMSO
%
% Tween 80
% ddH2O
%DMSO
%
計算結果：
投与溶媒濃度： mg/ml;
DMSOストック溶液調製方法： mg 試薬を μL DMSOに溶解する（濃度 mg/mL, 注：濃度が当該ロットのDMSO溶解度を超える場合はご連絡ください。 )
投与溶媒調製方法：Take μL DMSOストック溶液に μL PEG300，を加え、完全溶解後μL Tween 80，を加えて完全溶解させた後 μL ddH2O，を加え完全に溶解させます。
投与溶媒調製方法：μL DMSOストック溶液に μL Corn oil，を加え、完全溶解。
注意：１.ストック溶液に沈殿、混濁などがないことをご確認ください；
２.順番通りに溶剤を加えてください。次のステップに進む前に溶液に沈殿、混濁などがないことを確認してから加えてください。ボルテックス、ソニケーション、水浴加熱など物理的な方法で溶解を早めることは可能です。
技術サポート
ストックの作り方、阻害剤の保管方法、細胞実験や動物実験の際に注意すべき点など、製品を取扱う時に問い合わせが多かった質問に対しては取扱説明書でお答えしています。
他に質問がある場合は、お気軽にお問い合わせください。
* 必須
よくある質問（FAQ）
質問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.
Tags: Dactolisib (BEZ235)を買う | Dactolisib (BEZ235) ic50 | Dactolisib (BEZ235)供給者 | Dactolisib (BEZ235)を購入する | Dactolisib (BEZ235)費用 | Dactolisib (BEZ235)生産者 | オーダーDactolisib (BEZ235) | Dactolisib (BEZ235)化学構造 | Dactolisib (BEZ235)分子量 | Dactolisib (BEZ235)代理店
納期 国内在庫品：受注日の翌日（15時までの受注分） ＊北海道、九州、沖縄への配送は受注日より２日以上 を要する場合あり 海外在庫品：受注後１〜２週間