LGX818 is a selective ATP-competitive RAF kinase inhibitor of B-RafV600E 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). At oral doses of 6 mg/kg in human melanoma xenograft models, LGX818 was shown to decrease phosphorylation of the B-Raf substrate MEK.

Keywords: LGX818 | Supplier | RAF inhibitor | Encorafenib | NVP-LGX818 | LG-X818 | LGX 818 | NVPLGX818 | NVP LGX818 | CT-LGX818 | CAS [1269440-17-6] | MEK | RAF | Inhibitor | Enzymes