Afuresertib-GSK2110183C-DataSheet-生命科學(xué)試劑-MedChemExpress

1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemEAfuresertibCat. No.: HY-15727CAS No.: 1047644-62-1Synonyms: GSK2110183C分式: CHClFNOS分量: 427.32作靶點(diǎn): Akt作通路: PI3K/Akt/mTOR儲(chǔ)存式: -20C, protect from light, stored under nitrogen* In solvent : -80C, 6 months; -20C, 1 month (protect fro

2、mlight, stored under nitrogen)溶解性數(shù)據(jù)體外實(shí)驗(yàn) DMSO : 40 mg/mL (93.61 mM)* means soluble, but saturation unknown.Mass Solvent1 mg 5 mg 10 mg Concentration制備儲(chǔ)備液1 mM 2.3402 mL 11.7008 mL 23.4017 mL5 mM 0.4680 mL 2.3402 mL 4.6803 mL10 mM 0.2340 mL 1.1701 mL 2.3402 mL請根據(jù)產(chǎn)品在不同溶劑中的溶解度，選擇合適的溶劑配制儲(chǔ)備液，并請注意儲(chǔ)備液的保存式和期限

3、。BIOLOGICAL ACTIVITY物活性 Afuresertib種有效的 ATP 競爭性的特異性 Akt 抑制劑。IC50 & Target Akt體外研究Afuresertib exhibits favorable tumor-suppressive effects on malignant pleural mesothelioma (MPM) cells.Afuresertib significantly increases caspase-3 and caspase-7 activities and apoptotic cell number among1/2 Master of

4、Small Molecules 您邊的抑制劑師www.MedChemEACC-MESO-4 and MSTO-211H cells. Afuresertib strongly arrests the cell cycle in the G1 phase. Westernblotting analysis shows that Afuresertib increases the expression of p21WAF1/CIP1 and decreases thephosphorylation of Akt substrates, including GSK-3 and FOXO family

5、 proteins. Afuresertib-induced p21expression promotes G1 phase arrest by inducing FOXO activity. Afuresertib significantly enhances cisplatin-induced cytotoxicity. Afuresertib modulates the expression E2F1 and MYC, which are associated withfibroblast core serum response 1.PROTOCOLCell Assay 1 MPM ce

6、lls are seeded in 96-well plates (cell density, 2.5103 cells/well) and are incubated for 24 h at 37C.Next, the cells are incubated in a medium containing indicated concentrations of Akt inhibitors (e.g.,Afuresertib ; 50, 20, 10, 5, 2, 1, 0.5, 0.2, 0.1, and 0.01 M) for 72 h. Next, MTT solution is add

7、ed to each well,and the cells are incubated for 4 h. Finally, the cells are incubated overnight with lysis buffer (10% SDS in0.01 mol/L hydrogen chloride). Absorbance is measured at 550 nm using SpectraMAX M5spectrophotometer 1.MCE has not independently confirmed the accuracy of these methods. They

8、are for reference only.戶使本產(chǎn)品發(fā)表的科研獻(xiàn) Cell Syst. 2018 Apr 25;6(4):424-443.e7. Int J Cancer. 2019 Aug 7. J Physiol. 2017 Jul 1;595(13):4207-4225.See more customer validations on HYPERLINK / www.MedChemEREFERENCES1. Yamaji M, et al. Novel ATP-competitive Akt inhibitor Afuresertib suppresses the proliferation of malignant pleural mesothelioma cells.Cancer Med. 2017 Nov;6(11):2646-2659.McePdfHeightCaution: Product has not been fully validated for medical applicat