4-[(3-Bromophenyl)amino]-6-acrylamidoquinazoline Orange-yellow solid. PROTECT FROM LIGHT. PACKAGED UNDER INERT GAS. A potent, cell-permeable, irreversible, and selective inhibitor of EGF receptor (EGFR) tyrosine kinase activity (IC50 = 700 pM). Does not inhibit other protein kinases. Acts by binding to the catalytic domain of the EGFR with a 1:1 stoichiometry and alkylating Cys773. Excellent antitumor agent in vivo. Purity: ≥95% by HPLC. Ref.: Fry, D.W., et al. 1998. Proc. Natl. Acad. Sci USA 95, 12022. |