BMS-214662 mesylate is a potent and selective farnesyl transferase inhibitor with an IC50 of 1.35 nM. It exhibits antitumor activity and is applicable in cancer research.

BMS-214662 demonstrates selectivity for farnesyltransferase that exceeds 1000-fold, with IC50 values for inhibiting Ras-CVLL and K-Ras geranylgeranylation at 1.3 and 2.3 μM respectively [1]. It shows strong efficacy in inhibiting H-ras transformed rodent cells, A2780 human ovarian cancer cells, and HCT-116 human colon cancer cells. BMS-214662 is among the most potent apoptosis-inducing FTIs known, exhibiting broad-spectrum but highly selective cytotoxic activity across a range of cell lines with different histologies [2].

The administration of BMS-214662 in mice resulted in an increased number of apoptotic cells in their tumors, compared to untreated controls. In particular, BMS-214662 treatment elevated the apoptosis index (AI) in HCT-116 tumors by 4 to 10 times compared to untreated controls. BMS-214662 showed significant cytotoxic effects on both HCT-116 and EJ-1 tumor cells; specifically, the doses required to eliminate 90% of the clonogenic tumor cells were approximately 75 mg/kg for HCT-116 and 100 mg/kg for EJ-1 tumors [2].