BMS-214662|cas 195987-41-8

BMS-214662|cas 195987-41-8

DC Chemicals, Website: www.dcchemicals.com

Product Name: BMS-214662|Cas Number: 195987-41-8| Catalog Number: DC10200|Other Nmaes: BMS214662; BMS 214662

BMS-214662 is a potent and selective farnesyl transferase inhibitor with potent antitumor activity with an IC50 of 1.35 nM.

BMS-214662 is over 1000-fold selective for farnesyl transferase, having IC50 values for inhibition of geranylgeranylation of Ras-CVLL and K-Ras of 1.3 and 2.3 μM, respectively[1]. 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[2].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[2].