Chemical inhibition of EGFR signaling by BI 4732 in Caco-2 colorectal cancer cells.

Abstract

Colorectal cancer (CRC) is a major health problem worldwide, and treatment has not been sufficiently successful. EGFR inhibitors are one of the treatment options used in CRC therapy; however, due to developing resistance, there is a need for next-generation inhibitors. This study investigated how BI 4732, a next-generation EGFR inhibitor, affects WST-1 viability, colony formation, migration, soft agar, and 3D spheroid formation capabilities in Caco-2 cells. BI 4732 was found to inhibit viability in Caco-2 cells in a dose-dependent manner (IC50 983 ± 4.78 nM), significantly reduced colony formation at 40 and 80 nM treatment (p < 0.05 and p < 0.01, respectively), decreased the cells' mobilization ability (p < 0.01), and significantly inhibited soft agar colony formation and spheroid formation (p < 0.05). These results provide important preclinical data demonstrating the high in vitro efficacy of BI 4732 in the Caco-2 cell line.