| Identification | Back Directory | [Name]
(R)-1-((1H-IMidazol-4-yl)Methyl)-3-benzyl-4-(thiophen-2-ylsulfonyl)-2,3,4,5-tetrahydro-1H-benzo[e][1,4]diazepine-7-carbonitrile hydrochloride | [CAS]
195981-08-9 | [Synonyms]
BMS-214662monoHCl
BMS-214662 hydrochloride
-3-benzyl-4-(thiophen-2-ylsulfonyl)
BMS-214662 hydrochloride >=98% (HPLC)
-2,3,4,5-tetrahydro-1H-benzo[e][1,4]diazepine-7-carbonitrile hydrochloride
(R)-7-Cyano-2,3,4,5-tetrahydro-1-(1H-imidazol-4-ylmethyl)-3-(phenylmethyl)-4-(2-thienylsulfonyl)-1H-1,4-benzodiazepine, monohydrochloride
(R)-1-((1H-IMidazol-4-yl)Methyl)-3-benzyl-4-(thiophen-2-ylsulfonyl)-2,3,4,5-tetrahydro-1H-benzo[e][1,4]diazepine-7-carbonitrile hydrochloride | [Molecular Formula]
C25H24ClN5O2S2 | [MDL Number]
MFCD21604092 | [MOL File]
195981-08-9.mol | [Molecular Weight]
526.073 |
| Hazard Information | Back Directory | [Uses]
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]. | [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]. | [References]
[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. DOI:10.1021/jm000248z
[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. PMID:11606387 |
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