BMS-214662 mesylate

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BMS-214662 mesylate Basic information
Product Name:BMS-214662 mesylate
Synonyms:BMS-214662 mesylate;(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 methanesulfonate
CAS:474010-58-7
MF:C26H27N5O5S3
MW:585.71
EINECS:
Product Categories:
Mol File:474010-58-7.mol
BMS-214662 mesylate Structure
BMS-214662 mesylate Chemical Properties
Safety Information
MSDS Information
BMS-214662 mesylate Usage And Synthesis
UsesBMS-214662 mesylate is a potent and selective farnesyl transferase inhibitor with an IC50 of 1.35 nM. BMS-214662 mesylate exhibits potent antitumor activity and can be utilized in cancer research[1].
in vivo

Tumors from BMS-214662-treated mice have increased numbers of apoptotic cells as compared with the nontreated control mice. 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 75 and 100 mg/kg for HCT-116 and EJ-1 tumors[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
BMS-214662 mesylate Preparation Products And Raw materials
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