BMS-214662
- CAS号:195987-41-8
- 英文名:(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
- 中文名:BMS-214662
- CBNumber:CB81871450
- 分子式:C25H23N5O2S2
- 分子量:489.61
- MOL File:195987-41-8.mol
- 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: slightly soluble; Methanol: slightly soluble
- 形态 :A solid
- 酸度系数(pKa) :13.19±0.10(Predicted)
- 颜色 :White to off-white
BMS-214662性质、用途与生产工艺
- 生物活性 BMS-214662是有效选择性的farnesyl transferase抑制剂，具有有效地抗肿瘤活性。
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靶点
IC50: 1.35 nM (farnesyl transferase), 1.3 μM (Ras-CVLL), 2.3 μM (K-Ras)
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体外研究
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.
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体内研究
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.
- 公司名称：CLEARSYNTH LABS LTD.
- 联系电话：--
- 电子邮件：sales@clearsynth.com
- 国家：印度
- 产品数：6257
- 优势度：58
