PLX4720 is a potent and selective inhibitor of B-RafV600E with IC50 of 13 nM, equally potent to c-Raf-1(Y340D and Y341D mutations), 10-fold selectivity for B-RafV600E than wild-type B-Raf.

The Raf kinases activate cellular pathways that lead to cell proliferation and can contribute to certain types of cancer.Mutations in the kinase B-raf (BRAF) are involved in a wide range of cancers.In particular, the mutation BRAFV600E occurs in melanomas and thyroid cancer but is poorly targeted by many inhibitors of wild type BRAF.PLX4720 is an orally-available, highly selective inhibitor of BRAFV600E (IC50 = 13 nM).It is less effective against wild type BRAF (IC50 = 160 nM) as well as several other kinases.PLX4720 induces cell cycle arrest and apoptosis in cells and xenografts expressing the mutant of BRAF.