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CEP-32496

CEP-32496 is a kinase inhibitor that has multikinase binding activity but remains selectively cytotoxic for mutant (V600E) B-Raf (versus WT); it exhibits anticancer chemotherapeutic activity. Also contributing to the ability of CEP-32496 to inhibit cell proliferation, this compound inhibits pMEK and mERK in animal models with tumors containing the mutant B-Raf.

References PubMed ID::http://www.ncbi.nlm.nih.gov/pubmed/18848868

Cas No.

1188910-76-0

Purity

≥98%

Formula

C24H22F3N5O5

Formula Wt.

517.46

Chemical Name

Urea, N-[3-[(6,7-dimethoxy-4-quinazolinyl)oxy]phenyl]-N-[5-(2,2,2-trifluoro-1,1-dimethylethyl)-3-isoxazolyl]-

IUPAC Name

1-[3-(6,7-dimethoxyquinazolin-4-yl)oxyphenyl]-3-[4-(1,1,1-trifluoro-2-methylpropan-2-yl)-1,2-oxazol-3-yl]urea

Solubility

DMSO 9 mg/mL

Appearance

White to off white powder

James J, Ruggeri B, Armstrong RC, et al. CEP-32496: a novel orally active BRAF(V600E) inhibitor with selective cellular and in vivo antitumor activity. Mol Cancer Ther. 2012 Apr;11(4):930-41. PMID: 22319199.

Rowbottom MW, Faraoni R, Chao Q, et al. Identification of 1-(3-(6,7-dimethoxyquinazolin-4-yloxy)phenyl)-3-(5-(1,1,1-trifluoro-2-methylpropan-2-yl)isoxazol-3-yl)urea hydrochloride (CEP-32496), a highly potent and orally efficacious inhibitor of V-RAF murine sarcoma viral oncogene homologue B1 (BRAF) V600E. J Med Chem. 2012 Feb 9;55(3):1082-105. PMID: 22168626.

BMS-354825