STX-721

Description

STX-721 is an orally active, irreversible, covalent EGFR exon 20 insertion ex20ins inhibitor that selectively targets ex20ins-mutant dynamic protein states. STX-721 potently inhibits the kinase activity of EGFR ex20ins mutants NPG, ASV, SVD . STX-721 inhibits phosphorylation of EGFR pEGFR Y1068 and downstream ERK pERK Thr202/Tyr204 , and suppresses proliferation of ex20ins-mutant Ba/F3 cells and human NSCLC cell lines NCI-H2073 ASV KI, CUTO-14 ASV . STX-721 induces tumor regression in EGFR ex20ins-mutant PDX/CDX models. STX-721 can be used for the study of non-small cell lung cancer NSCLC harboring EGFR or HER2 ex20ins mutations.