CAS 1010085-13-8 | MK-5108 (VX-689) Highly Selective Aurora A Inhibitor

Chemical properties: 

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MK-5108 is a highly selective Aurora A inhibitor with IC50 of 0.064 nM in a cell-free assay, showing 220-fold and 190-fold selectivity for Aurora A over Aurora B/C, and less than 100-fold selectivity for TrkA. MK-5108 (VX-689) induces autophagy. (Phase 1)

In VITRO STUDIES: MK-5108 inhibits Aurora-A activity in an ATP-competitive manner with an IC50 value of 0.064 nM. It shows strong selectivity over other family kinases Aurora-B (220-fold) and Aurora-C (190-fold). MK-5108 is also selective 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 STUDIES: MK-5108 treatment at 15 and 30 mg/kg resulted in significant tumor growth inhibition in the HCT116 tumor model. MK-5108 was well tolerated at both doses, with minimal weight loss. MK-5108 also showed significant antitumor activity in SW48 tumor-bearing nude mice. MK-5108 at 15 and 45 mg/kg caused dose-dependent tumor growth inhibition with %T/C of 35% and 7% on day 10 and 58% and 32% on day 27, respectively. MK-5108 was well tolerated in nude mice, with no weight loss and moderate effects on blood cells.

(Alfa has not independently confirmed the accuracy of these methods. They are for reference only.)

production method: N/A

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