Description
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
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.