AZD1152-HQPA (722544-51-6) is a potent and highly selective inhibitor of Aurora B.¹ Aurora B K_i = 0.36 nM; Aurora A K_i = 1,369 nM.² It inhibits the growth of tumors in multiple cancer models.^3-6 Excessive ROS generation⁷ and upregulated tumor suppressor miRNAs⁸ have been proposed as a novel mechanisms of cytotoxicity of AZD1152-HQPA.

References/Citations
1) Mortlock et al. (2007) Discovery, Synthesis, and in Vivo Activity of a New Class of Pyrazoloquinazolines as Selective Inhibitors of Aurora B Kinase; J. Med. Chem. 50 2213
2) Wilkinson et al. (2007) AZD1152, a Selective Inhibitor of Aurora B Kinase, Inhibits Human Tumor Xenograft Growth by Inducing Apoptosis; Clin. Cancer Res. 13 3682
3) Oke et al. (2009) AZD1152 rapidly and negatively affects the growth and survival of human acute myeloid leukemia cells in vitro and in vivo; Cancer Res. 69 4150
4) Aihara et al. (2010) The selective Aurora B kinase inhibitor AZD1152 as a novel treatment for hepatocellular carcinoma; J. Hepatol. 52 63
5) Mori et al. (2011) Effects of AZD1152, a selective Aurora B kinase inhibitor of Burkitt’s and Hodgkin’s lymphomas; Biochem. Pharmacol. 82 1252
6) Helfrich et al. (2016) Barasertib (AZD1152), a Small Molecule Aurora B Inhibitor, Inhibits the Growth of SCLC Cell Lines In Vitro and In Vivo; Mol. Cancer Ther. 15 2314
7) Zekri et al. (2017) Reactive oxygen species generation and increase in mitochondrial copy number: new insight into the potential mechanism of cytotoxicity induced by aurora kinase inhibitor, AZD1152-HQPA; Anticancer Drugs 28 841
8) Zekri et al. (2018) The Potential Contribution of microRNAs in Anti-cancer Effects of Aurora Kinase Inhibitor (AZD1152-HQPA); J. Mol. Neurosci. 65 444