Catalog No.: PC-62100Not For Human Use, Lab Use Only.
Avapritinib (BLU-285) is a potent and highly selective inhibitor of mutant KIT and PDGFRα with IC50 of 0.6, 0.27 and 0.24 nM for KIT del557-558, KIT D816V and PDGFRA D842V, respectively.
Avapritinib (BLU-285) is a potent and highly selective inhibitor of mutant KIT and PDGFRα with IC50 of 0.6, 0.27 and 0.24 nM for KIT del557-558, KIT D816V and PDGFRA D842V, respectively.
Avapritinib (BLU-285) displays weak inhibition against WT KIT with IC50 of 73 nM, >150-fold more potent on KIT D816V than several important kinase antitargets such as VEGFR2, SRC and FLT3.
Avapritinib (BLU-285) inhibits other well-characterized disease-driving KIT mutants both in vitro and in vivo in preclinical models.
Avapritinib (BLU-285) demonstrates marked activity in patients with diseases associated with KIT and PDGFRA (GIST) activation loop mutations.
