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

BMS-214662化学性质

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。
靶点

IC50: 1.35 nM (farnesyl transferase), 1.3 μM (Ras-CVLL), 2.3 μM (K-Ras)
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.
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.

BMS-214662上下游产品信息

上游原料

下游产品

BMS-214662生产厂家