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| Cas No.: | 1047644-62-1 |
| Chemical Name: | Afuresertib |
| Synonyms: | GSK-2110183;GSK 2110183;N-[(1S)-2-Amino-1-[(3-fluorophenyl)methyl]ethyl]-5-chloro-4-(4-chloro-1-methyl-1H-pyrazol-5-yl)-2-thiophenecarboxamide;GSK 2110183C;Delitinib;Afuresertib;GSK-2110183C;Afuresertib(GSK2110183C);Afuresertib, GSK-2110183, GSK-2110183B;N-((S)-1-amino-3-(3-fluorophenyl)propan-2-yl)-5-chloro-4-(4-chloro-1-methyl-1H-pyrazol-5-yl)thiophene-2-carboxamide;GSK2110183;GSK2110183C;Afuresertib free base;Afuresertib (GSK2110183);ASB183;8739X25QI3;Afuresertib HCl;2-Thiophenecarboxamide, N-((1S)-2-amino-1-((3-fluorophenyl)methyl)ethyl)-5-chloro-4-(4-chloro-1-methyl-1H-pyrazol-5-yl)-;N-[(2S)-1-amino-3-(3-fluorophenyl)propan-2-yl]-5-chloro-4-(4-chloro-2-methyl-3-pyrazolyl)-2-thiophenecarboxamide;Afuresertib [USAN:INN];Afuresertib (USAN) |
| SMILES: | ClC1=C(C2=C(C([H])=NN2C([H])([H])[H])Cl)C([H])=C(C(N([H])[C@]([H])(C([H])([H])N([H])[H])C([H])([H])C2C([H])=C([H])C([H])=C(C=2[H])F)=O)S1 |
| Formula: | C18H17Cl2FN4Os |
| M.Wt: | 427.3232 |
| Purity: | >98% |
| Sotrage: | 2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO |
| Description: | Afuresertib is a potent and ATP-competitive specific Akt inhibitor. |
| In Vitro: | 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 among ACC-MESO-4 and MSTO-211H cells. Afuresertib strongly arrests the cell cycle in the G1 phase. Western blotting analysis shows that Afuresertib increases the expression of p21WAF1/CIP1 and decreases the phosphorylation of Akt substrates, including GSK-3β and FOXO family proteins. Afuresertib-induced p21 expression promotes G1 phase arrest by inducing FOXO activity. Afuresertib significantly enhances cisplatin-induced cytotoxicity. Afuresertib modulates the expression E2F1 and MYC, which are associated with fibroblast core serum response[1]. |
| Cell Assay: | MPM cells are seeded in 96-well plates (cell density, 2.5×103 cells/well) and are incubated for 24 h at 37°C. 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 μM) for 72 h. Next, MTT solution is added to each well, and the cells are incubated for 4 h. Finally, the cells are incubated overnight with lysis buffer (10% SDS in 0.01 mol/L hydrogen chloride). Absorbance is measured at 550 nm using SpectraMAX M5 spectrophotometer[1]. |
| References: | [1]. 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. |
MSDS
COA
| LOT NO. | DOWNLOAD |
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| 2018-0101 |
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| 2018-0101 |
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