MK-8745
Catalog No.S7065
Molecular Weight(MW): 431.91
MK-8745 is a potent and selective Aurora A inhibitor with IC50 of 0.6 nM, more than 450-fold selectivity for Aurora A over Aurora B.
Purity & Quality Control
Choose Selective Aurora Kinase Inhibitors
Biological Activity
| Description | MK-8745 is a potent and selective Aurora A inhibitor with IC50 of 0.6 nM, more than 450-fold selectivity for Aurora A over Aurora B. | ||
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| Targets |
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| In vitro |
MK-8745 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. Treatment with MK-8745 induces p21(waf1/cip1) and CycB1, indicating cell cycle arrest and an increase in the G2/M phase cell population. Following MK-8745 treatment, Aurora-A substrates (TACC3, Eg5 and TPX2) are rapidly degraded following the reduction of phospho-Aurora-A. [1] MK8745 induces apoptotic cell death in a p53-dependent manner when tested in vitro in cell lines of multiple lineages. Exposure of p53 wild-type cells to MK8745 results in the induction of p53 phosphorylation (ser15) and an increase in p53 protein expression. p53-dependent apoptosis by MK8745 is further confirmed in HCT 116 p53(-/-) cells transfected with wild-type p53. [2] |
Protocol
Solubility (25°C)
| In vitro | DMSO | 86 mg/mL (199.11 mM) |
|---|---|---|
| Ethanol | 1 mg/mL (2.31 mM) | |
| Water | Insoluble |
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
Chemical Information
| Molecular Weight | 431.91 |
|---|---|
| Formula | C20 H19 Cl F N5 O S |
| CAS No. | 885325-71-3 |
| Storage | powder |
| in solvent | |
| Synonyms | N/A |
Bio Calculators
Molarity Calculator
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* When preparing stock solutions always use the batch-specific molecular weight of the product found on the vial label and MSDS / COA (available online).
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Molarity Calculator
Tech Support
Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.
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