SB-699393 is a potent, selective and CNS penetrant B-Raf inhibitor with Kd of 7.2 nM; possesses enhanced CNS penetration (BB ratio=0.8:1) compared with SB-590885.
BGB-283 (Lifirafenib, BGB283) is a potent pan RAF inhibitor of BRAF V600E, wt BRAF, CRAFY340/341D and wt ARAF (IC50=5-40 nM); inhibits recombinant BRAFV600E with IC50 of 23 nM; also inhibits EGFR and EGFR T790M/L858R with IC50 of 29 nM and 495 nM respectively; potently inhibits BRAF(V600E)-activated ERK phosphorylation and cell proliferation in vitro; shows tumor growth inhibition in both cell line-derived and primary human colorectal tumor xenografts bearing BRAF(V600E) mutation.
AZ 628(AZ-628, AZ628) is a potent and selective B-Raf inhibitor with IC50s of 2.14 uM and 0.19 uM for wt Braf and Braf V600E respectively.
Phase 1 Clinical
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