AZD1152-HQPA
Aurora B kinase inhibitor / AZD1152-HQPA is a potent and highly selective inhibitor of Aurora B.1 Aurora B Ki = 0.36 nM; Aurora A Ki = 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.
Biochemicals & reagents
722544-51-6
Barasertib-HQPA; AZD2811
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
-20°C
TARGET: Kinase -- PATHWAY: Cytotoxicity -- RESEARCH AREA: Oxidative stress; Cell death -- DISEASE AREA: Cancer