A potent inhibitor of Aurora kinases
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MK-5108

Item No. 19167

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
trans-4-(3-chloro-2-fluorophenoxy)-1-[[6-(2-thiazolylamino)-2-pyridinyl]methyl]-cyclohexanecarboxylic acid
CAS Number
1010085-13-8
Synonyms
  • VX-689
Molecular Formula
C22H21ClFN3O3S
Formula Weight
461.9
Purity
≥95%
Formulation (Request formulation change)
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMF: 5 mg/mlDMF:PBS (pH7.2) (1:30): 0.025 mg/mlDMSO: 2 mg/ml
λmax
278, 310 nm
SMILES
ClC1=C(F)C(O[C@@H]2CC[C@@](CC3=CC=CC(NC4=NC=CS4)=N3)(C(O)=O)CC2)=CC=C1
InChi Code
InChI=1S/C22H21ClFN3O3S/c23-16-4-2-5-17(19(16)24)30-15-7-9-22(10-8-15,20(28)29)13-14-3-1-6-18(26-14)27-21-25-11-12-31-21/h1-6,11-12,15H,7-10,13H2,(H,28,29)(H,25,26,27)/t15-,22-
InChi Key
LCVIRAZGMYMNNT-VVONHTQRSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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Certificates of Analysis & Batch Specific Data

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    1 mg

    $63

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    5 mg

    $274

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    10 mg

    $481

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    Product Description

    MK-5108 is a potent inhibitor of Aurora A (IC50 = 0.064 nM).1 It less potently inhibits Aurora B and Aurora C (IC50s =14 and 12 nM, respectively). MK-5108 blocks cell cycle progression and induces apoptosis in a diverse range of human tumor types.1,2 It is effective in vivo, inhibiting the growth of xenograft tumors in mice.1

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Harrington, E.A., Bebbington, D., Moore, J., et al. VX-680, a potent and selective small-molecule inhibitor of the Aurora kinases, suppresses tumor growth in vivo. Nat. Med. 10(3), 262-267 (2004).

    2. Shimmoura, T., Hasako, S., Nakatsuru, Y., et al. MK-5108, a highly selective Aurora-A kinase inhibitor, shows antitumor activity alone and in combination with docetaxel. Mol. Cancer Ther. 9(1), 157-166 (2010).