CP-724714 is a quinazoline-based, orally-available, ATP-competitive inhibitor of erbB2 at an IC50 of 10 nM, with exquisite selectivity over EGFR kinase (6.4 uM) and >1000-fold selectivity over IR, IGFR, PDGFRb, VEGFR2, Abl, Src, cMet, JNK, CDK2, and CDK5. [1] CP-724714 is a potent inhibitor of erbB2 autophosphorylation (EC50 = 1 ug/mL) and induces G1 cell cycle arrest with concomitant reduction in S-phase cells. [1]

CP-724714 exhibits linear single-dose and multiple-dose pharmacokinetics. [2], but was discontinued from clinical development due to unexpected hepatotoxicity. [3]