EGFR-IN-60

Description

EGFR-IN-60 Compound 7d shows obvious inhibition of EGFRWT, EGFRT790M, EGFRL858R and JAK3 with IC50s of 83, 26, 53, and 69 nM, respectively. EGFR-IN-60 potently inhibits the growth of H1975 cells harboring EGFRT790M mutation IC50=1.32 AAasAasAAmuM over A431 cells overexpressing EGFRWT IC50=4.96 AAasAasAAmuM . EGFR-IN-60 exhibits good oral absorption, potent and safe antitumor activity. EGFR-IN-60 induces cell death through apoptosis supported by increased Bax/Bcl-2 ratio.