EGFR-HER2 Ex20Ins inhibitor 1a is a highly potent, broadly effective EGFR and HER2 Exon 20 insertion mutant inhibitor with biochemical IC50 of <0.5 nM (wtEGFR, 100 uM ATP).
EGFR-HER2 Ex20Ins inhibitor 1a is a highly potent, broadly effective EGFR and HER2 Exon 20 insertion mutant inhibitor with biochemical IC50 of <0.5 nM (wtEGFR, 100 uM ATP).
EGFR-HER2 Ex20Ins inhibitor 1a exhibits superior inhibition of proliferation and signaling pathways in Ba/F3 cells harboring either EGFR or HER2 Ex20Ins mutations (IC50=7.5-35 nM), and in the EGFR P772_H773insPNP patient-derived lung cancer cell line DFCI127 compared with afatinib.
EGFR-HER2 Ex20Ins inhibitor 1a induces a dose-dependent reduction of EGFR and Erk phosphorylation in EGFR InsSVD transformed Ba/F3 cells with strong inhibition at 0.1 uM.
EGFR-HER2 Ex20Ins inhibitor 1a displays broad and superior antiproliferative activities against EGFR and HER2 Ex20Ins mutants than currently approved 2nd and 3rd generation irreversible EGFR inhibitors.
