|
Biological Activity:
AZD 1152-HQPA is a highly potent and selective inhibitor of Aurora B, with Ki values to be 0.36 (Aurora B) and 1369 nM (Aurora A) respectively and has a high specificity versus a panel of 50 other kinases. The dihydrogen phosphate prodrug, AZD 1152 (Barasertib), is converted rapidly to active AZD1152-HQPA in plasma.
References:
RW Wilkinson et al. AZD1152, a Selective Inhibitor of Aurora B Kinase, Inhibits Human Tumor Xenograft Growth by Inducing Apoptosis. Clin. Cancer Res. 2007 13(12), 3682-3688. [online]
N Keen et al. Biological characterisation of AZD1152, a highly potent and selective inhibitor of aurora kinase activity. Clin. Cancer Res. 2005, 11, B220.
E Walsby et al. Effects of the aurora kinase inhibitors AZD1152-HQPA and ZM447439 on growth arrest and polyploidy in acute myeloid leukemia cell lines and primary blasts. Haematologica 2008, 93(5), 662-669. [online]
Y Tao et al. Enhancement of radiation response in p53-deficient cancer cells by the Aurora-B kinase inhibitor AZD1152. Oncogene 2008, 27, 3244-3255. [online]
Chemical Name: 2-[5-(7-{3-[Ethyl-(2-hydroxy-ethyl)-amino]-propoxy}-quinazolin-4-ylamino)-1H-pyrazol-3-yl]-N-(3-fluoro-phenyl)-acetamide
| 
