MK-8745

Catalog No.S7065

For research use only.

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.

MK-8745 Chemical Structure

CAS No. 885325-71-3

Purity & Quality Control

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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.
Targets
Aurora A [1]
()
0.6 nM
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 (from reference)

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 3 years -20°C powder
2 years -80°C in solvent
Smiles C1CN(CCN1CC2=NC(=CC=C2)NC3=NC=CS3)C(=O)C4=C(C(=CC=C4)Cl)F

In vivo Formulation Calculator (Clear solution)

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%DMSO %

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Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Molarity Calculator

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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.

Handling Instructions

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