Biological Activity of LGX818

LGX818 is an orally available mutated BRaf V600E inhibitor(IC50=0.3 nM) with potential antineoplastic activity.
IC50 value: 0.3 nM (BRaf V600E biochemical); 2 nM (A375 cell proliferation) [1]
Target: mutated BRaf V600E
LGX818 is a drug candidate for the treatment of melanoma with the V600E mutation in the B-RAF kinase. The substance is being developed by Novartis, is in phase III clinical trials, and was disclosed at the spring 2013 American Chemical Society meeting in New Orleans. More information can be found in Patent WO2011025927A1

References on LGX818

[1]. Compounds and compositions as protein kinase inhibitors . Patent WO 2011025927 A1

[2]. LGX818, From Wikipedia, the free encyclopedia