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MK-5108

Chemical Structure : MK-5108

CAS No.: 1010085-13-8

MK-5108 (MK 5108;VX-689;VX 689;MK5108;VX689)

Catalog No.: PC-43431Not For Human Use, Lab Use Only.

MK-5108 (VX-689) is a potent, highly selective Aurora-A kinase inhibitor with IC50 of 0.064 nM.

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5 mg $88 In stock
10 mg $128 In stock
25 mg $198 In stock
50 mg $328 In stock
100 mg $548 In stock
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Purity & Documentation Purity: >98% (HPLC) Select Batch:

Biological Activity

MK-5108 (VX-689) is a potent, highly selective Aurora-A kinase inhibitor with IC50 of 0.064 nM, displays robust selectivity against Aurora-B (220-fold) and Aurora-C (190-fold) in the biochemical assays.
MK-5108 (VX-689) also exhibits high selectivity for Aurora-A over a panel of 233 kinases, only one kinase (TrkA) with <100-fold selectivity.
MK-5108 (VX-689) inhibits the growth of multiple human cancer cell lines in vitro and in human cancer xenograft models.
MK-5108 (VX-689) MK-5108 significantly enhanced the efficacy of docetaxel without increasing its toxicity.

Physicochemical Properties

M.Wt 461.94
Formula C22H21ClFN3O3S
Appearance Solid
CAS No.
Storage
Solide Powder
-20 °C 12 Months; 4°C 6 Months
In Solvent
-80 °C 6 Months; -20°C 6 Months
Shipping
Solubility

DMSO: 6.4 mg/mL (Need warming)

Chemical Name/SMILES

Cyclohexanecarboxylic acid, 4-(3-chloro-2-fluorophenoxy)-1-[[6-(2-thiazolylamino)-2-pyridinyl]methyl]-, trans-

References

1. Shimomura T, et al. Mol Cancer Ther. 2010 Jan;9(1):157-66.

2. Kretzner L, et al. Cancer Res. 2011 Jun 1;71(11):3912-20.

3. Shan W, et al. Clin Cancer Res. 2012 Jun 15;18(12):3352-65.

4. Chefetz I, et al. Cell Cycle. 2011 Jul 1;10(13):2206-14.

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