BIEGi-1 is a potent and selective EGFR dimerization inhibitor that effectively blocks EGFR-catalyzed nucleotide exchange and disrupts the EGFR-Rheb interaction. It strongly inhibits EGFR kinase activity and mTORC1 signaling in EGFR-mutant cancer cells. BIEGi-1 exhibits significant antiproliferative effects, with an IC50 of 17 nM against [PC9] and an IC50 of 20 nM against [HCC827].