CHMFL-EGFR-26 irreversibly inhibits EGFR kinase via formation a covalent bond with Cys797 residue in a distinct DFG-in-cHelix-out inactive conformation of EGFR and displays good in vitro and in vivo anti-NSCLC efficacies in the preclinical models. This evidence concerns the gene EGFR and non-small cell lung carcinoma.