MK-5108 free base · Synonyms: VX-689

MK-5108 is a highly potent and specific inhibitor of Aurora A kinase.

For research use only. Not for human or veterinary use.

Target Aurora Kinase Autophagy

Research area Cancer

Purity >98% Stock Inquire

Data Sheet SDS COA

MK-5108 structure

CAS No.: 1010085-13-8

Download structure (.mol)

Pack sizes & pricing

Size	Price	SKU	Stock
100 mg	USD 430.00	BP-02297-100mg	In stock	Get quote
250 mg	USD 850.00	BP-02297-250mg	In stock	Get quote
500 mg	USD 1,350.00	BP-02297-500mg	In stock	Get quote
1 g	USD 2,170.00	BP-02297-1g	In stock	Get quote
2 g	USD 3,480.00	BP-02297-2g	In stock	Get quote
3 g	USD 4,170.00	BP-02297-3g	In stock	Get quote
5 g	Inquire	BP-02297-5g	In stock	Inquire
10 g	Inquire	BP-02297-10g	In stock	Inquire

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Description

MK-5108 is a highly potent and specific inhibitor of Aurora A kinase with an IC50 value of 0.064 nM.

Biological activity

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.

Identifiers

SMILES: OC(=O)[C@@]1(CC2=NC(NC3=NC=CS3)=CC=C2)CC[C@@H](CC1)OC1=CC=CC(Cl)=C1F
InChIKey: LCVIRAZGMYMNNT-VVONHTQRSA-N

Specifications

MW (average): 461.9370
Formula: C₂₂H₂₁ClFN₃O₃S
CAS No.: 1010085-13-8
Physical state: Solid
Color: White to off-white
Shipping: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage: Powder -20℃ 3 years; In solvent -20℃ 1 month;

Solubility

Soluble in DMSO

Documents

References

[1]. Shimomura T, et al. MK-5108, a highly selective Aurora-A kinase inhibitor, shows antitumor activity alone and in combination with docetaxel. Mol Cancer Ther. 2010 Jan;9(1):157-66.

Same target

Search Aurora Kinase

Same research area

Search Cancer