BMS-214662 is an effective and selective inhibitor of farnesyl transferase with potent antitumor activity (IC50: 1.35 nM).

BMS-214662 is over 1000-fold selective for farnesyl transferase, having IC50 values for inhibition of geranylgeranylation of K-Ras and Ras-CVLL of 2.3 and 1.3 μM, respectively [1]. BMS-214662 shows good potency in inhibiting A2780 human ovarian carcinoma tumor cells, H-ras-transformed rodent cells, and HCT-116 human colon carcinoma tumor cells. BMS-214662 is a potent apoptotic FTI and demonstrates broad-spectrum yet robust cell-selective cytotoxic activity against a panel of cell lines with diverse histology [2].

As compared with the nontreated control mice, Tumors from BMS-214662-treated mice have increased numbers of apoptotic cells. 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 100 and 75 mg/kg for EJ-1 and HCT-116 tumors [2].

195987-41-8

C25H23N5O2S2

489.61

DMSO:100 mg/mL (204.24 mM)
Powder: -20°C for 3 years
In solvent: -80°C for 2 years