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Cat. No. Name Size Price Add Cart
KI0604MK-51085 mg$432
MK-510810 mg$592
MK-510850 mg$1712
MK-5108200 mg$3952

Chemical Characteristic

Product NameMK-5108
SynonymsVX-689
CAS No.1010085-13-8
Molecular Weight 461.94
FormulaC22H21CLFN3O3S
Chemical Nametrans-4-(3-Chloro-2-fluorophenoxy)-1-[[6-(2-thiazolylamino)-2-pyridinyl]methyl]cyclohexanecarboxylic acid
Smiles[C@]1(CC[C@@H](CC1)Oc1c(c(ccc1)Cl)F)(C(=O)O)Cc1cccc(n1)Nc1sccn1
Chemical Structure

Biological activities

MK-5108 is a potent and selective Aurora A inhibitor with IC50 of 0.064 nM. MK-5108 inhibits Aurora-A activity in an ATP-competitive manner. MK-5108 has robust selectivity against the Aurora-B (220-fold) and Aurora-C (190-fold) in the biochemical assay. MK-5108 inhibits only one kinase (TrkA) with <100-fold selectivity. In syn-chronized HeLa-S3 cells, MK-5108 treatment (300 nM-10 µM) induces accumulation of pHH3-positive cells. Consistent with the induction of pHH3-positive cells, MK-5108 induces accumulation of cells in the G2-M phase in asynchronously cultured HeLa-S3 cells. MK-5108 inhibits the proliferation of breast tumor cell lines HCC1143, AU565, MCF-7, and HCC1806 with IC50 values of 0.42, 0.45, 0.52, and 0.56 µM, respectively. MK-5108 inhibits the proliferation of colon tumor cell lines HCT116, Colo205, and SW48 with IC50 values of 0.27, 0.5, and 0.16 µM, respectively.[1] MK-5108 induces phosphorylated Histone H3 in skin and xenograft tumor tissues in a nude rat xenograft model. MK-5108 inhibits tumor growth in different xenograft models. Furthermore, the combination of MK-5108 and docetaxel shows enhanced antitumor activities compared with control and docetaxel alone-treated animals without exacerbating the adverse effects of docetaxel.[1] In vitro, combining MK-5108 with vorinostat enhances lymphoma cell killing with repression of c-Myc, hTERT, and microRNA levels.[2] Gavage of an orthotopic ULMS model with MK-5108 ( 30 or 60 mg/kg) decreases the number and size of tumor implants compared with sham-fed controls. Oral MK-5108 also decreases the rate of proliferation, increases intratumoral apoptosis, and increases expression of phospho-histone H3 in ULMS xenografts.[3]

Protocols

In vitro: MK-5108 is dissolved in DMSO.[2]

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, 9(1): 157-166.
[2] Kretzner L, et al. 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, 71(11): 3912-3920.
[3] Shan W, et al. A small-molecule inhibitor targeting the mitotic spindle checkpoint impairs the growth of uterine leiomyosarcoma. Clin Cancer Res. 2012, 18(12): 3352-3365.

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