Avapritinib (BLU-285) II-SC

Avapritinib (BLU-285) II-SCAvapritinib (BLU 285) is a small molecule kinase inhibitor that potently inhibits PDGFR? D842V mutant activity in vitro (IC50 = 0. 5 nM) and PDGFR? D842V autophosphorylation in the cellular setting (IC50 = 30 nM); also a potent inhibitor of the analogous KIT mutation, D816V in KIT Exon 17 (IC50 = 0. 5 nM).

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and allosteric inhibitor of oncogenic K-Ras(G12C)

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is a potent and highly selective inhibitor of UGT1A4 with an IC50 value of 1

while exhibiting no inhibitory action on other kinases including PI3K

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also inhibits angiogenesis and tumor dormancy through suppressing vascular endothelial growth factor (VEGF) gene transcription

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