An orally available, third generation, selective inhibitor of mutant forms of the epidermal growth factor receptor (EGFR), including the second-site resistance mutation T790M, with potential antineoplastic activity. EGFR mutant-selective inhibitor AC0010MA specifically and irreversibly binds to and inhibits the activity of mutant forms of EGFR, which prevents EGFR mutant-mediated signaling and leads to cell death in EGFR mutant-expressing tumor cells. Compared to some other EGFR inhibitors, AC0010MA may have therapeutic benefits in tumors with T790M-mediated drug resistance. This agent does not inhibit wild-type EGFR (EGFRwt), and does not cause dose-limiting toxicities that occur during the use of non-selective EGFR inhibitors, which also inhibit EGFRwt. EGFR, a receptor tyrosine kinase mutated in many tumor cell types, plays a key role in tumor cell proliferation and tumor vascularization.