MK-5108,1010085-13-8

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MK-5108

CAS No. : 1010085-13-8

MCE 国际站：MK-5108

产品活性：MK-5108是高效和特异性的极光激酶A抑制剂，IC₅₀ 值为0.064 nM。

研究领域：Cell Cycle/DNA Damage  |  Epigenetics  |  Autophagy

作用靶点：Aurora Kinase  |  Autophagy

In Vitro: MK-5108 inhibits Aurora-A activity with an IC₅₀ value of 0.064 nM in an ATP-competitive manner. It shows robust selectivity against the other family kinases Aurora-B (220-fold) and Aurora-C (190-fold). MK-5108 also exhibits high selectivity for Aurora-A over other protein kinases. MK-5108 inhibits the growth of 14 cell lines with IC₅₀ values between 0.16 and 6.4 μM.

In Vivo: MK-5108 treatments at 15 and 30 mg/kg results in significant tumor growth inhibition in the HCT116 tumor model. MK-5108 is well tolerated at both doses, with minimal reduction in body weight. MK-5108 also exhibits significant antitumor activity in nude rats bearing SW48 tumors. MK-5108 at 15 and 45 mg/kg causes dose-dependent tumor growth inhibition with a %T/C of 35% and 7% at day 10, and 58% and 32% at day 27, respectively. MK-5108 is well tolerated in nude rats, with no body weight reduction and moderate effect on blood cells.

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