MK-8745 - Aurora Kinase 抑制剂 - 生命科学试剂 - MedChemExpress

1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemEMK-8745Cat. No.: HY-13819CAS No.: 885325-71-3分式: CHClFNOS分量: 431.91作靶点: Aurora Kinase作通路: Cell Cycle/DNA Damage; Epigenetics储存式: Powder -20C 3 years4C 2 yearsIn solvent -80C 6 months-20C 1 month溶解性数据体外实验 DMSO : 100 mg/mL (231.53

2、 mM)* means soluble, but saturation unknown.Mass Solvent1 mg 5 mg 10 mg Concentration制备储备液1 mM 2.3153 mL 11.5765 mL 23.1530 mL5 mM 0.4631 mL 2.3153 mL 4.6306 mL10 mM 0.2315 mL 1.1576 mL 2.3153 mL请根据产品在不同溶剂中的溶解度，选择合适的溶剂配制储备液，并请注意储备液的保存式和期限。体内实验请根据您的实验动物和给药式选择适当的溶解案，配制前请先配制澄清的储备液，再依次添加助溶剂(为保证实验结果的可靠性，

3、体内实验的作液，建议您现现配，当天使；澄清的储备液可以根据储存条件，适当保存；以下溶剂前的百分 指该溶剂在您配制终溶液中的体积占)：1. 请依序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% salineSolubility: 2.5 mg/mL (5.79 mM); Clear solution2. 请依序添加每种溶剂： 10% DMSO 90% (20% SBE-CD in saline)Solubility: 2.5 mg/mL (5.79 mM); Clear solution3. 请依序添加每种溶剂： 10% DMSO 90% corn oil

4、1/2 Master of Small Molecules 您边的抑制剂师www.MedChemESolubility: 2.5 mg/mL (5.79 mM); Clear solutionBIOLOGICAL ACTIVITY物活性 MK-8745是极光激酶抑制剂 (aurora A)，IC50 值为0.6 nM。IC50 & Target Aurora A0.6 nM (IC50)体外研究 MK-8745 induces apoptotic cell death in a p53-dependent manner when tested in vitro in cell lines of

5、 multiplelineages. Exposure of p53 wild-type cells to MK-8745 results in the induction of p53 phosphorylation (ser15)and an increase in p53 protein expression 1. 1 M of MK-8745 exposure for 24 h induces cell cycle arrest inall NHL cells, with variable degrees of G2/M arrest. Z138C cells are highly s

6、ensitive to MK-8745 (1 M)treatment and induces an approximate 5.5-fold increase in the G2/M phase cell population by 96 h. MK-8745treatment inhibits phosphorylation of Aurora-A in Granta 519 and Z138C cells, while Akata and JVM2 has noeffect. MK-8745 specifically inhibits Aurora-A specific function.

7、 MK-8745 treatment leads to apoptotic celldeath 2.PROTOCOLCell Assay 2 A total of 10000 cells are plated per well in a 96-well plate and treated with MK-8745 for varying time pointsstarting 24 h after plating. Cell viability is measured by the MTT assay 2.MCE has not independently confirmed the accu

8、racy of these methods. They are for reference only.户使本产品发表的科研献 Sci Transl Med. 2018 Jul 18;10(450). pii: eaaq1093. J Cell Sci. 2019 Jun 12. pii: jcs.229385.See more customer validations on HYPERLINK / www.MedChemEREFERENCES1. Jayasree S Nair et al. The induction of polyploidy or apoptosis by the Aur

9、ora 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-Hodgkinlymphoma cell lines.Leuk Lymphoma, 2012 Mar, 53(3):462-71.McePdfHeightCaution: Product has not been fully validated for medical