BLU-285 (Avapritinib)|exon 17 mutant KIT inhibitor

BLU-285 (Avapritinib)|exon 17 mutant KIT inhibitor

DC Chemicals, Website: www.dcchemicals.com

Product Name: BLU-285 (Avapritinib)|Cas Number: 1703793-34-3| Catalog Number: DC10530|Other Nmaes: BLU-285,BLU 285,BLU285

BLU-285 is a potent and selective exon 17 mutant KIT kinase inhibitor with IC50 of 0.27 nM for KIT D816V.

BLU-285 has demonstrated biochemical in vitro activity on the KIT exon 17 mutant enzyme, KIT D816V (IC50=0.27 nM). Cellular activity of BLU-285 on KIT D816 mutants is measured by autophosphorylation in the human mast cell leukemia cell line HMC1.2, and the P815 mouse mastocytoma cell line with IC50=4 and 22 nM, respectively. In Kasumi-1 cells, a t(8;21)-positive AML cell line with a KIT exon 17 N822K mutation, BLU-285 potently inhibits KIT N822K mutant autophosphorylation (IC50=40 nM), downstream signaling, as well as cellular proliferation (IC50=75 nM).