BMS-214662 (hydrochloride)

BMS-214662 hydrochloride is an inhibitor of farnesyltransferase (Farnesyl Transferase). BMS-214662 hydrochloride can effectively block the localization and function of Ras proteins on the cell membrane by inhibiting the prenylation modification of Ras proteins, thereby exerting anti-tumor activity. The IC₅₀ value of BMS-214662 hydrochloride for H-Ras is 1.3 nM, and for K-Ras it is 8.4 nM. BMS-214662 hydrochloride can be used in the research of tumor diseases related to Ras^[1][2]. IC50 & Target:IC50: 1.35 nM (farnesyl transferase), 1.3 μM (Ras-CVLL), 2.3 μM (K-Ras)^[1] In Vitro:BMS-214662 has over 1000 times selectivity for farnesyltransferase, with IC₅₀ values for inhibiting geranylgeranylation of Ras-CVLL and K-Ras at 1.3 and 2.3 μM, respectively^[1]. BMS-214662 demonstrates 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 effective apoptotic FTI known and exhibits broad-spectrum but robust cell-selective cytotoxic activity against a panel of cell lines with diverse histology^[2]. In Vivo:Compared to untreated control mice, the number of apoptotic cells in tumors from mice treated with BMS-214662 increased. The Apoptotic Index (AI) in HCT-116 tumors from BMS-214662-treated mice increased by 4-10 times compared to the untreated control group. BMS-214662 exhibited significant cytotoxicity against HCT-116 and EJ-1 tumor cells; the doses of BMS-214662 required to kill 90% of clonogenic tumor cells were approximately 75 and 100 mg/kg for HCT-116 and EJ-1 tumors, respectively^[2].