1、MK-8745Cat. No.: HY-13819CAS No.: 885325-71-3Molecular Formula: CHClFNOSMolecular Weight: 431.91Target: Aurora KinasePathway: Cell Cycle/DNA Damage; EpigeneticsStorage: Powder -20C 3 years4C 2 yearsIn solvent -80C 6 months-20C 1 monthSolvent & SolubilityIn Vitro DMSO : 34 mg/mL (78.72 mM)* “ means s
2、oluble, but saturation unknown.ConcentrationSolvent Mass 1 mg 5 mg 10 mg1 mM 2.3153 mL 11.5765 mL 23.1530 mL5 mM 0.4631 mL 2.3153 mL 4.6306 mLPreparing Stock Solutions10 mM 0.2315 mL 1.1576 mL 2.3153 mLPlease refer to the solubility information to select the appropriate solvent.BIOLOGICAL ACTIVITYDe
3、scription MK-8745 is an aurora A kinase inhibitor with IC50s of 0.6 nM.IC & Target Aurora A, IC50: 0.6 nMIn Vitro MK-8745 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 MK-8745 results in the inductio
4、n of p53 phosphorylation (ser15) and an increase in p53 protein expression1. 1 M of MK-8745 exposure for 24 h induces cell cycle arrest in all NHL cells, with variable degrees of G2/M arrest. Z138C cells are highly sensitive to MK-8745 (1 M) treatment and induces an approximate 5.5-fold increase in
5、the G2/M phase cell population by 96 h. MK-8745 treatment inhibits phosphorylation of Aurora-A in Granta 519 and Z138C cells, while Akata and JVM2 has no effect. MK-8745 specifically inhibits Aurora-A specific function. MK-8745 treatment leads to apoptotic cell death2.Product Data Sheet InhibitorsAg
6、onistsScreening Librarieswww.MedChemE1PROTOCOLCell Assay 2 A total of 10000 cells are plated per well in a 96-well plate and treated with MK-8745 for varying time points starting 24 h after plating. Cell viability is measured by the MTT assay2.MCE has not independently confirmed the accuracy of thes
7、e methods. They are for reference only.REFERENCES1. Jayasree S Nair et al. The induction of polyploidy or apoptosis by the Aurora A kinase inhibitor MK8745 is p53-dependent.2. Aparajita Chowdhury et al. A novel Aurora kinase A inhibitor MK-8745 predictsTPX2 as a therapeutic biomarker in non-Hodgkin lymphoma cell lines.Leuk Lymphoma, 2012 Mar, 53(3):462-71.Caution: Product has not been fully validated for medical applications. For research use only.Tel: 609-228-6898 Fax: 609-228-5909 E-mail: techMedChemEAddress: 1 Deer Park Dr, Suite Q, Monmouth Junction, NJ 08852, USAwww.MedChemE2
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