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MK-8745 is a novel and selective inhibitor of Aurora A with IC50 value of 0.6 nM [1].

Aurora A kinase is a member of mitotic serine/threonine kinases and plays an important role in cellular division by controlling chromatid segregation. It has been reported that abnormal expression of Aurora A is correlated with the high occurrence of cancer and its expression determines cell sensitivity to MK-8745 treatment [1].

MK-8745 is a potent Aurora A inhibitor. When tested with p53-/+ cell lines, MK-8745 treatment induced apoptotic cell death in a p53-dependent manner through inhibiting Aurora A activity [1]. In non-Hodgkin lymphoma (NHL) cell lines, MK-8745 treatment arrested cell cycle in G2/M phase and induced cell death via inhibiting Aurora A kinase [2]. In HCT 116 Puma (-), HCT116 p21 (-), HCT116 Bax(-) and HCT116 Chk2(-) cell lines, MK-8745 treatment induced cell apoptosis with the percent of 25%, 22%, 25%, and 22%, respectively [3].

In female athymic nude mice model subcutaneous xenografted with HCT116 Puma (-), HCT116 p21 (-), HCT116 Bax(-) and HCT116 Chk2(-) cells, administration of MK-8745 significantly inhibited tumor growth [3].

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