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Description: MK-8745 is a novel, potent, specific and selective Aurora A inhibitor with potential antitumor activity. It inhibits Aurora A with an IC50 of 0.6 nM, and is 450-fold more selective for Aurora A over Aurora B. It shows potent in vitro antiproliferative activity and high in vivo antitumor efficacy. Exposure of p53 wild-type cells to MK8745 resulted in the induction of p53 phosphorylation (ser15) and an increase in p53 protein expression. p53-dependent apoptosis by MK8745 was further confirmed in HCT 116 p53(-/-) cells transfected with wild-type p53.
References: Leuk Lymphoma. 2012 Mar; 53(3):462-71; Cell Cycle. 2012 Feb 15; 11(4):807-17.
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