MK-5108
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MedKoo CAT#: 525687

CAS#: 1010085-13-8

Description: MK-5108, also known as VX689, is a novel small molecule with potent inhibitory activity against Aurora-A kinase. MK-5108 specifically inhibited Aurora-A kinase in a panel of protein kinase assays. MK-5108 also induced phosphorylated Histone H3 in skin and xenograft tumor tissues in a nude rat xenograft model. MK-5108 inhibited growth of human tumor cell lines in culture and in different xenograft models. MK-5108 is currently tested in clinical trials and offers a new therapeutic approach to combat human cancers as a single agent or in combination with existing taxane therapies. (source: Mol Cancer Ther. 2010 Jan;9(1):157-66. Epub 2010 Jan 6.).


Price and Availability

Size
Price

500mg
USD 2850
5g
Ask price
Size
Price

1g
USD 3650
Size
Price

2g
USD 5650

MK-5108, purity > 98%, is in stock. Minimum 500mg order. Current shipping out time is about 2 weeks after order is received. CoA, QC data and MSDS documents are available in one week after order is received. Delivery time: overnight (USA/Canada); 3-5 days (worldwide). Shipping fee: from $30.00 (USA); from $45.00 (Canada); from $70.00 (international). Note: Lead time for order of > 1g may be 2-3 months.


Chemical Structure

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Theoretical Analysis

MedKoo Cat#: 525687
Name: MK-5108
CAS#: 1010085-13-8
Chemical Formula: C22H21ClFN3O3S
Exact Mass: 461.09762
Molecular Weight: 461.94
Elemental Analysis: C, 57.20; H, 4.58; Cl, 7.67; F, 4.11; N, 9.10; O, 10.39; S, 6.94


Synonym: MK5108; MK-5108; MK 5108; VX689; VX 689; VX-689.

IUPAC/Chemical Name: (1r,4r)-4-(3-chloro-2-fluorophenoxy)-1-((6-(thiazol-2-ylamino)pyridin-2-yl)methyl)cyclohexane-1-carboxylic acid

InChi Key: LCVIRAZGMYMNNT-VVONHTQRSA-N

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-

SMILES Code: O=C([C@@]1(CC2=NC(NC3=NC=CS3)=CC=C2)CC[C@H](OC4=CC=CC(Cl)=C4F)CC1)O


Technical Data

Appearance:
Solid powder

Purity:
>98% (or refer to the Certificate of Analysis)

Shipping Condition:
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 Condition:
Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).

Solubility:
soluble in DMSO, not soluble in water.

Shelf Life:
>5 years if stored properly

Drug Formulation:
This drug may be formulated in DMSO

Stock Solution Storage:
0 - 4 C for short term (days to weeks), or -20 C for long term (months).

Harmonized System Code:
293490


Additional Information

 
 
 


References

1: Shan W, Akinfenwa PY, Savannah KB, Kolomeyevskaya N, Laucirica R, Thomas DG, Odunsi K, Creighton CJ, Lev DC, Anderson ML. A small-molecule inhibitor targeting the mitotic spindle checkpoint impairs the growth of uterine leiomyosarcoma. Clin Cancer Res. 2012 Jun 15;18(12):3352-65. Epub 2012 Apr 25. PubMed PMID: 22535157.

2: Chefetz I, Holmberg JC, Alvero AB, Visintin I, Mor G. Inhibition of Aurora-A kinase induces cell cycle arrest in epithelial ovarian cancer stem cells by affecting NFĸB pathway. Cell Cycle. 2011 Jul 1;10(13):2206-14. Epub 2011 Jul 1. PubMed PMID: 21623171; PubMed Central PMCID: PMC3154367.

3: Kretzner L, Scuto A, Dino PM, Kowolik CM, Wu J, Ventura P, Jove R, Forman SJ, Yen Y, Kirschbaum MH. Combining histone deacetylase inhibitor vorinostat with aurora kinase inhibitors enhances lymphoma cell killing with repression of c-Myc, hTERT, and microRNA levels. Cancer Res. 2011 Jun 1;71(11):3912-20. Epub 2011 Apr 18. PubMed PMID: 21502403; PubMed Central PMCID: PMC3107377.

4: Shimomura T, Hasako S, Nakatsuru Y, Mita T, Ichikawa K, Kodera T, Sakai T, Nambu T, Miyamoto M, Takahashi I, Miki S, Kawanishi N, Ohkubo M, Kotani H, Iwasawa Y. 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. Epub 2010 Jan 6. PubMed PMID: 20053775.

5: Lok W, Klein RQ, Saif MW. Aurora kinase inhibitors as anti-cancer therapy. Anticancer Drugs. 2010 Apr;21(4):339-50. Review. PubMed PMID: 20016367.