474010-58-7

Name	BMS-214662 mesylate
CAS	474010-58-7
Molecular Formula	C26H27N5O5S3
MDL Number	MFCD21608670
Molecular Weight	585.71
MOL File	474010-58-7.mol

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

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Hazard Information

Uses

BMS-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

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