Avapritinib CAS# 1703793-34-3 阿泊替尼

Avapritinib is a selective, orally available small-molecule inhibitor of KIT and PDGFRA receptor tyrosine kinases, with strongest activity against PDGFRA exon 18 mutations, including the D842V substitution. In vitro studies demonstrate potent inhibition of mutant KIT/PDGFRA signaling, leading to suppression of downstream proliferative pathways and induction of apoptosis in tumor cells. In vivo, avapritinib reduces tumor burden and prolongs survival in xenograft models of gastrointestinal stromal tumors (GIST), supporting its therapeutic use in advanced or resistant disease settings.