EGFR-IN-109 (compound 4), an EGFR inhibitor, displays IC 50 values of 25.8 nM for EGFR WT and 182.3 nM for EGFR T790M. This compound halts the growth of cancer cells at the G2/M phase and triggers both early and late apoptosis. It is applicable in cancer research [1].

EGFR:25.8 nM, EGFR T790M:182.3 nM

EGFR-IN-109 (compound 4) effectively inhibits the proliferation of high EGFR-expressing MCF-7 and A549 cells with IC50 values of 13.06 μM and 20.13 μM, respectively, over 2 days [1]. At a concentration of 13.06 μM for 24 hours, this compound induces apoptosis in A549 cells by arresting cell growth at the G2/M phase [1]. Additionally, a 72-hour exposure at 13.06 μM enhances the expression of caspase-3, caspase-9, and BAX proteins, while downregulating Bcl-2 expression in A549 cells [1]. In a cell proliferation assay involving MCF-7, A549, and normal W138 cell lines, EGFR-IN-109 at concentrations ranging from 0-20 μM demonstrated a pronounced inhibitory effect on MCF-7 and A549, and a weaker effect on WI-38 cells, with selectivity indices of 2.8 and 1.8 for the two cancer cell lines, respectively.