(3-chloro-2-fluorophenyl)(4-((6-(thiazol-2-ylamino)pyridin-2-yl)methyl)piperazin-1-yl)methanone. MK-8745
MK-8745
CAS: 885325-71-3
Molecular Formula: C20H19ClFN5OS
(3-chloro-2-fluorophenyl)(4-((6-(thiazol-2-ylamino)pyridin-2-yl)methyl)piperazin-1-yl)methanone. MK-8745 - Names and Identifiers
(3-chloro-2-fluorophenyl)(4-((6-(thiazol-2-ylamino)pyridin-2-yl)methyl)piperazin-1-yl)methanone. MK-8745 - Physico-chemical Properties
| Molecular Formula | C20H19ClFN5OS |
| Molar Mass | 431.91 |
| Density | 1.430±0.06 g/cm3(Predicted) |
| Melting Point | 177-179°C |
| Boling Point | 605.5±65.0 °C(Predicted) |
| Solubility | DMSO: ≥ 34 mg/mL |
| Appearance | Solid |
| Color | Off-White |
| pKa | 5.20±0.10(Predicted) |
| Storage Condition | Refrigerator |
| Use | The MK-8745 is an aurora kinase inhibitor (aurora A) with an IC50 value of 0.6 nM. |
| Target | Aurora A Aurora B |
| In vitro study | In non-Hodgkin's lymphoma (NHL) cell lines, MK-8745 leads to cell cycle arrest at the G2/ M phase with aggregation of tetraploid nuclei followed by cell death. MK-8745 induced p21(WAF1/CIP1) and CYCB1, indicating cell cycle arrest and increased G2/M phase cell population. MK-8745 treatment resulted in rapid degradation of Aurora-A substrates (TACC3, Eg5, and TPX2) followed by a decrease in phosphorylation Aurora-A. When in vitro in a variety of cell lines, MK8745 induces apoptotic cell death in a p53-dependent manner. In p53 wild-type cells, MK8745 induces p53 phosphorylation (ser15) and increases the expression of p53 protein. P53-dependent apoptosis of MK8745 transfected with wild-type p53 in HCT 116 p53(-/-) cells was further confirmed. |
(3-chloro-2-fluorophenyl)(4-((6-(thiazol-2-ylamino)pyridin-2-yl)methyl)piperazin-1-yl)methanone. MK-8745 - Reference
| Reference Show more | 1. Chowdhury, A., S. Chowdhury, M.Y., et al. Tsai, A novel Aurora kinase A inhibitor MK-8745 predicts TPX2 as a therapeutic biomarker in non-Hodgkin lymphoma cell lines. Leuk Lymphoma, 2012. 53(3): p. 462-712. Shionome, Y., et al. Integrity of p53 associated pathways determines induction of apoptosis of tumor cells resistant to Aurora-A kinase inhibitors. PLoS One, 2013. 8(1): p. e55457. |
(3-chloro-2-fluorophenyl)(4-((6-(thiazol-2-ylamino)pyridin-2-yl)methyl)piperazin-1-yl)methanone. MK-8745 - Preparation solution concentration reference
| 1mg | 5mg | 10mg | |
|---|---|---|---|
| 1 mM | 2.315 ml | 11.576 ml | 23.153 ml |
| 5 mM | 0.463 ml | 2.315 ml | 4.631 ml |
| 10 mM | 0.232 ml | 1.158 ml | 2.315 ml |
| 5 mM | 0.046 ml | 0.232 ml | 0.463 ml |
Last Update：2024-01-02 23:10:35
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