Afuresertib (hydrochloride)
Modify Date: 2024-01-07 00:06:09
Afuresertib (hydrochloride) structure
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Common Name | Afuresertib (hydrochloride) | ||
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| CAS Number | 1047645-82-8 | Molecular Weight | 463.78400 | |
| Density | N/A | Boiling Point | N/A | |
| Molecular Formula | C18H18Cl3FN4OS | Melting Point | N/A | |
| MSDS | N/A | Flash Point | N/A | |
Use of Afuresertib (hydrochloride)Afuresertib hydrochloride is a potent and ATP-competitive specific Akt inhibitor. |
| Name | N-[(2S)-1-amino-3-(3-fluorophenyl)propan-2-yl]-5-chloro-4-(4-chloro-2-methylpyrazol-3-yl)thiophene-2-carboxamide,hydrochloride |
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| Synonym | More Synonyms |
| Description | Afuresertib hydrochloride is a potent and ATP-competitive specific Akt inhibitor. |
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| Related Catalog | |
| Target |
Akt |
| 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 |
| Molecular Formula | C18H18Cl3FN4OS |
|---|---|
| Molecular Weight | 463.78400 |
| Exact Mass | 462.02500 |
| PSA | 101.18000 |
| LogP | 5.78750 |
| Storage condition | 2-8℃ |
| Afuresertib HCl |
| Afuresertib hydrochloride |
| UNII-0FC27E442O |
| GSK2110183 |
| Afuresertib (hydrochloride) |