EGFR/VEGFR2-IN-10 is a selective inhibitor of EGFR, VEGFR2, and COX2 with IC50 values of 8.5, 68, and 158 nM, respectively. This compound can induce G1 phase cell cycle arrest in MCF-7 cells. EGFR/VEGFR2-IN-10 increases the Bax/Bcl-2 ratio, upregulates caspase-8 expression, and elevates caspase-9 protein levels, thereby activating the intrinsic apoptotic pathway. It demonstrates favorable selectivity by inhibiting tumor proliferation, angiogenesis, and inflammation pathways. EGFR/VEGFR2-IN-10 serves as a tool for the study of cervical cancer, liver cancer, colon cancer, and breast cancer.

EGFR:8.5 nM

EGFR/VEGFR2 IN 10 exhibits antitumor activity against various cancer cell lines, with IC₅₀ values of 4.93 μM for Hela, 2.34 μM for HepG2, 6.07 μM for HCT 116, and 3.35 μM for MCF 7, achieving selectivity indices (SI) of 16.86, 11.78, 8.00, and 6.50, respectively, and demonstrating lower cytotoxicity to normal WI 38 cells (IC₅₀ = 39.45 μM). At a concentration of 3.35 μM over 48 hours, EGFR/VEGFR2-IN-10 blocks cell cycle progression at the G1 checkpoint in MCF-7 cells and induces programmed cell death. It promotes a selective anticancer mechanism in MCF 7 breast cancer cells through dual actions: effectively inducing apoptosis in both early and late stages without causing necrosis or related inflammatory responses; simultaneously enhancing pro-apoptotic signals and suppressing anti-apoptotic defenses to overcome apoptotic resistance.