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: 1.35 nM (farnesyl transferase), 1.3 μM (Ras-CVLL), 2.3 μM (K-Ras)^[1]

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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

526.07

C₂₅H₂₄ClN₅O₂S₂

195981-08-9

N#CC1=CC=C(N(CC2=CN=CN2)C[C@@H](CC3=CC=CC=C3)N(S(=O)(C4=CC=CS4)=O)C5)C5=C1.Cl

Room temperature in continental US; may vary elsewhere.

Please store the product under the recommended conditions in the Certificate of Analysis.

• [1]. Hunt JT, et al. Discovery of (R)-7-cyano-2,3,4, 5-tetrahydro-1-(1H-imidazol-4-ylmethyl)-3- (phenylmethyl)-4-(2-thienylsulfonyl)-1H-1,4-benzodiazepine (BMS-214662), a farnesyltransferase inhibitor with potent preclinical antitumor activity. J Med Chem. 2000 Oct 5;43(20):3587-95.  [Content Brief]

  [2]. Rose WC, et al. Preclinical antitumor activity of BMS-214662, a highly apoptotic and novel farnesyltransferase inhibitor. Cancer Res. 2001 Oct 15;61(20):7507-17.  [Content Brief]