The recurrent missense mutation T790M in the kinase domain of epidermal growth factor receptor (EGFR) is a gatekeeper mutation, as it sterically hinders binding of inhibitors while preserving catalytic activity. WZ4002 is an irreversible EGFR tyrosine kinase inhibitor that blocks ATP-dependent autophosphorylation of...

WZ4002 inhibits EGFR in a variety of cell lines, including those harboring the T790M gatekeeper mutation. WZ2004 exhibits anticancer chemotherapeutic activity, inhibiting proliferation of lung adenocarcinoma cells and suppressing tumor growth in animal models.