An ATP-competitive inhibitor of mutant V600E/F and wild type B-Raf, IC50s=31 and 100 nM respectively.1 Induced growth inhibition, G0/G1 arrest and apoptosis in a variety of cancer cell lines, with a B-Raf mutation favoring but not guaranteeing a response.2 Inhibits the growth of B-Raf V600E-positive melanomas in vitro and in vivo.3 Treatment of patients that carry the V600E BRAF mutation resulted in complete or partial tumor regression.4
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