Lifirafenib (BGB-283, BGB283) is a potent pan RAF inhibitor of BRAF V600E, wt BRAF, CRAFY340/341D and wt ARAF (IC50=5-40 nM).
BGB-283 (Lifirafenib) inhibits recombinant BRAFV600E with IC50 of 23 nM; also inhibits EGFR and EGFR T790M/L858R with IC50 of 29 nM and 495 nM respectively.
BGB-283 (Lifirafenib) potently inhibits BRAF(V600E)-activated ERK phosphorylation and cell proliferation in vitro.
BGB-283 (Lifirafenib) shows tumor growth inhibition in both cell line-derived and primary human colorectal tumor xenografts bearing BRAF(V600E) mutation.
