PLX-4720

BeschreibungThe Raf kinases activate cellular pathways that lead to cell proliferation and can contribute to certain types of cancer. Mutations in the kinase B-Raf are involved in a wide range of cancers. In particular, the mutation B-RafV600E occurs in melanomas and thyroid cancer but is poorly targeted by many inhibitors of wild type B-Raf. PLX4720 is an orally-available, highly selective inhibitor of B-RafV600E (IC50 = 13 nM). It is less effective against wild type B-Raf (IC50 = 160 nM) as well as several other kinases. PLX4720 induces cell cycle arrest and apoptosis in cells and xenografts expressing the mutant of B-Raf.