(1S)-1-(4-fluorophenyl)-1-[2-[4-[6-(1-methylpyrazol-4-yl)pyrrolo[2,1-f][1,2,4]triazin-4-yl]piperazin-1-yl]pyrimidin-5-yl]ethanamine BLU-285
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BLU-285 is a potent and selective inhibitor of exon 17 mutant KIT (IC50 = 0.27 nM for KIT D816V). BLU-285 showed dose-dependent, robust anti-tumor efficacy in a TKI-resistant KIT exon 11/17 mutant GIST PDX model through inhibition of tumor growth, proliferation, KIT signaling and induction of apoptosis.
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