ZM447439

ZM447439 is a potent and selective small-molecule inhibitor of the **Aurora kinase family**, particularly acting on **Aurora B kinase** with high affinity, and to a lesser extent on Aurora A and C kinases. It is a quinazoline derivative and was the first Aurora kinase inhibitor reported (2003). ZM447439 acts by targeting the ATP-binding site of Aurora kinases, competitively inhibiting phosphorylation of key substrates such as histone H3 (Ser10, Ser28). In vitro, it inhibits both Aurora A (AURKA) and Aurora B (AURKB), but in vivo it mainly inhibits AURKB. Mechanistically, inhibition of Aurora B kinase leads to **defects in chromosome alignment, segregation, cytokinesis, cell cycle arrest (G2/M), and induction of apoptosis via the p53-dependent mitochondrial pathway**. ZM447439 demonstrates anti-proliferative and pro-apoptotic effects in a variety of human and animal cancer cell lines and is investigational for its preclinical anti-tumor effects, including in gastroenteropancreatic neuroendocrine tumors (GEP-NETs) and lymphoid malignancies[1][4][8][10].

Other names

ZM 447439ZM447439ZM-447439N-[4-[[6-Methoxy-7-[3-(4-morpholinyl)propoxy]-4-quinazolinyl]amino]phenyl]benzamideCS-77CS77CS 77Aurora Kinase Inhibitor VI