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MK-5108 inhibits aurora kinase A (AurA) preventing mitotic spindle formation and proper completion of mitosis. MK-5108 exhibits anticancer chemotherapeutic activity. In uterine leiomyosarcoma cells, MK-5108 inhibits proliferation and induces apoptosis; in animal models, this compound decreases tumor number and size. Additionally, in epithelial ovarian cancer cells, MK-5108 induces polyploidy and cell cycle arrest, and inhibits activation of NF-κB.
| Cas No. | 1010085-13-8 |
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| Purity | ≥98% |
| Formula | C22H21ClFN3O3S • HCl |
| Formula Wt. | 498.39 |
| Chemical Name | MK-5108 Hydrochloride |
| IUPAC Name | 4-(3-chloro-2-fluorophenoxy)-1-[[6-(1,3-thiazol-2-ylamino)pyridin-2-yl]methyl]cyclohexane-1-carboxylic acid;hydrochloride |
| Synonym | MK5108, VX-689, VX689 |
| Solubility | Solubility in DMSO-12 mg/mL |
| Store Temp | -20°C |
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| Ship Temp | Ambient |
| MSDS | |
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| Info Sheet |
Shan W, Akinfenwa PY, Savannah KB, et al. 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. PMID: 22535157.
Chefetz I, Holmberg JC, Alvero AB, et al. 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. PMID: 21623171.