CP-724714

CP‑724,714 is an orally bioavailable small molecule inhibitor that selectively targets the Receptor tyrosine-protein kinase erbB‑2 (HER2). It is a quinazoline derivative with high potency (IC50 = 10 nM for HER2) and over 640-fold selectivity against other kinases such as EGFR, InsR, PDGFR, VEGFR2, Abl, Src, and c-Met[1][5]. The drug binds to the intracellular domain of HER2 and reversibly inhibits its tyrosine kinase activity. This leads to suppression of tumor cell growth by blocking downstream signaling pathways involved in cell proliferation and survival[5][4]. Preclinical studies demonstrated that CP‑724,714 induces G1 cell cycle arrest and apoptosis in HER2-overexpressing cancer cells. It was developed primarily for the treatment of cancers characterized by HER2 overexpression—most notably breast cancer—and entered clinical trials for breast cancer and metastatic neoplasms[3][5]. However, clinical development was discontinued due to unexpected hepatotoxicity observed in patients[6].

Other names

2-Methoxy-N-[3-[4-[3-methyl-4-[(6-methyl-3-pyridinyl)oxy]anilino]-6-quinazolinyl]prop-2-enyl]acetamide383432-38-0