BMS-214662
| 中文名称 | BMS-214662 |
|---|---|
| 中文同义词 | 化合物 T10567;(3R)-2,3,4,5-四氢-1-(1H-咪唑-5-基甲基)-3-(苯基甲基)-4-(2-噻吩基磺酰基)-1H-1,4-苯并二氮杂环庚烷-7-氰基 |
| 英文名称 | (4R)-4-benzyl-2-(3H-imidazol-4-ylmethyl)-5-thiophen-2-ylsulfonyl-2,5-diazabicyclo[5.4.0]undeca-8,10,12-triene-9-carbonitrile |
| 英文同义词 | (4R)-4-benzyl-2-(3H-imidazol-4-ylmethyl)-5-thiophen-2-ylsulfonyl-2,5-diazabicyclo[5.4.0]undeca-8,10,12-triene-9-carbonitrile;1H-1,4-Benzodiazepine-7-carbonitrile,2,3,4,5-tetrahydro-1-(1H-iMidazol-5-ylMethyl)-3-(phenylMethyl)-4-(2-thienylsulfonyl)-,(3R)-;(3R)-2,3,4,5-Tetrahydro-1-(1H-iMidazol-4-ylMethyl)-3-(phenylMethyl)-4-(2-thienylsulfonyl)-1H-1,4-benzodiazepine-7-carbonitrile;(R)-2,3,4,5-Tetrahydro-1-(1H-iMidazol-4-ylMethyl)-3-(phenylMethyl)-4-(2-thienylsulfonyl)-1H-1,4-benzodiazepine-7-ca;BMS214662; BMS 214662;7-Cyano-2,3,4,5-tetrahydro-1-(1H-imidazol-4-ylmethyl)-3-(phenylmethyl)-4-(2-thienylsulfonyl)-1H-1,4-benzodiazepine;(3R)-2,3,4,5-Tetrahydro-1-(1H-imidazol-5-ylmethyl)-3-(phenylmethyl)-4-(2-thienylsulfonyl)-1H-1,4-benzodiazepine-7-carbonitrile |
| CAS号 | 195987-41-8 |
| 分子式 | C25H23N5O2S2 |
| 分子量 | 489.61 |
| EINECS号 | |
| 相关类别 | Aromatics;Heterocycles;Inhibitors;Intermediates & Fine Chemicals;Pharmaceuticals;Sulfur & Selenium Compounds |
| Mol文件 | 195987-41-8.mol |
| 结构式 |  |
BMS-214662 性质
| 沸点 | 790.9±70.0 °C(Predicted) |
|---|---|
| 密度 | 1.45±0.1 g/cm3(Predicted) |
| 储存条件 | Store at -20°C |
| 溶解度 | DMSO：微溶；甲醇：微溶 |
| 形态 | 固体 |
| 酸度系数(pKa) | 13.19±0.10(Predicted) |
| 颜色 | 白色至米白色 |
IC50: 1.35 nM (farnesyl transferase), 1.3 μM (Ras-CVLL), 2.3 μM (K-Ras)
BMS-214662 is over 1000-fold selective for farnesyl transferase, having IC 50 values for inhibition of geranylgeranylation of Ras-CVLL and K-Ras of 1.3 and 2.3 μM, respectively. BMS-214662 shows good potency in inhibiting H-ras-transformed rodent cells, A2780 human ovarian carcinoma tumor cells, and HCT-116 human colon carcinoma tumor cells. BMS-214662 is the most potent apoptotic FTI known and demonstrates broad spectrum yet robust cell-selective cytotoxic activity against a panel of cell lines with diverse histology.
Tumors from BMS-214662-treated mice have increased numbers of apoptotic cells as compared with the nontreated control mice. The AIs in HCT-116 tumors are increased 4-10-fold in BMS-214662-treated mice as compared with nontreated controls. BMS-214662 is significantly cytotoxic to both HCT-116 and EJ-1 tumor cells; the doses of BMS-214662 required to kill 90% of clonogenic tumor cells are approximately 75 and 100 mg/kg for HCT-116 and EJ-1 tumors.