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…

A potent inhibitor of B-RafV600E (Kd = 14 nM in an in vitro binding assay); blocks B-RafV600E–dependent phosphorylation of MEK in human melanoma A375 and colorectal cancer COLO 205 cells (IC₅₀s = 78 and 60 nM, respectively); displays good oral bioavailability.