For research use only. Not for therapeutic Use.
MK-8745（Cat No.:I005315）is a selective inhibitor of Aurora A kinase, a crucial enzyme involved in the regulation of cell division. By inhibiting Aurora A, MK-8745 disrupts proper mitotic spindle formation, leading to mitotic arrest and apoptosis in cancer cells. This compound has shown potential in targeting cancer types with high Aurora A expression, making it a valuable tool for cancer research. MK-8745 is widely used to study cell cycle regulation, tumor progression, and the development of targeted therapies aimed at controlling cancer cell proliferation.
| Catalog Number | I005315 |
| CAS Number | 885325-71-3 |
| Synonyms | (3-chloro-2-fluorophenyl)(4-((6-(thiazol-2-ylamino)pyridin-2-yl)methyl)piperazin-1-yl)methanone |
| Molecular Formula | C₂₀H₁₉ClFN₅OS |
| Purity | ≥95% |
| Target | Aurora Kinase |
| Solubility | DMSO: 86 mg/mL; Ethanol: 1 mg/mL |
| Storage | Store at -20 C |
| IUPAC Name | (3-chloro-2-fluorophenyl)-[4-[[6-(1,3-thiazol-2-ylamino)pyridin-2-yl]methyl]piperazin-1-yl]methanone |
| InChI | InChI=1S/C20H19ClFN5OS/c21-16-5-2-4-15(18(16)22)19(28)27-10-8-26(9-11-27)13-14-3-1-6-17(24-14)25-20-23-7-12-29-20/h1-7,12H,8-11,13H2,(H,23,24,25) |
| InChIKey | YCRFPWKUUNKNDN-UHFFFAOYSA-N |
| SMILES | C1CN(CCN1CC2=NC(=CC=C2)NC3=NC=CS3)C(=O)C4=C(C(=CC=C4)Cl)F |
| Reference | 1:Leuk Lymphoma. 2012 Mar;53(3):462-71. doi: 10.3109/10428194.2011.619018. Epub 2011 Oct 24. A novel Aurora kinase A inhibitor MK-8745 predicts TPX2 as a therapeutic biomarker in non-Hodgkin lymphoma cell lines.Chowdhury A,Chowdhury S,Tsai MY, PMID: 21879811 DOI: 10.3109/10428194.2011.619018 </br><span>Abstract:</span> Selective small-molecule kinase inhibitors have encouraging clinical efficacy in several malignancies. These agents are still limited to a subset of patients, indicating the need to develop therapeutic biomarkers that influence clinical benefit. In this study, we demonstrate that treatment with MK-8745, a novel Aurora-A specific inhibitor, leads to cell cycle arrest at the G2/M phase with accumulation of tetraploid nuclei followed by cell death in non-Hodgkin lymphoma (NHL) cell lines. The sensitivity of the cell lines to MK-8745 is correlated with the expression level of Aurora-A activator. The siRNA knockdown of Aurora-A activator TPX2 (targeting protein for Xenopus kinase-like protein 2) increased MK-8745 sensitivity in less-MK-8745-sensitive NHL cell lines, whereas overexpression of TPX2 in high-MK-8745-sensitive NHL cell lines increased drug resistance. Our results indicate that TPX2 may serve as a biomarker for identifying subpopulations of patients sensitive to Aurora-A inhibitor treatment. |
