Cayman Encorafenib

B-Raf is a MAP kinase kinase kinase, which functions downstream of Ras family GTPases to activate MEK1/2 and ERK1/2 signaling. A mutation of B-Raf in exon 15 at codon 600 where a valine is substituted by glutamic acid (V600E) has been linked to melanoma.¹ Encorafenib is a selective inhibitor of B-Raf^V600E mutant melanoma cell proliferation (EC₅₀ = 4 nM) with little activity against wild-type B-Raf or a panel of 100 other kinases (IC₅₀s = 900 nM).² At oral doses of 6 mg/kg in human melanoma xenograft models, encorafenib was shown to decrease phosphorylation of the B-Raf substrate MEK.³

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