1047645-82-8
1047645-82-8 structure
- Name: Afuresertib (hydrochloride)
- Chemical Name: N-[(2S)-1-amino-3-(3-fluorophenyl)propan-2-yl]-5-chloro-4-(4-chloro-2-methylpyrazol-3-yl)thiophene-2-carboxamide,hydrochloride
- CAS Number: 1047645-82-8
- Molecular Formula: C18H18Cl3FN4OS
- Molecular Weight: 463.78400
- Catalog: Research Areas Cancer
- Create Date: 2017-02-02 05:32:00
- Modify Date: 2024-01-07 00:06:09
-
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 |
|---|---|
| Synonyms |
Afuresertib HCl
Afuresertib hydrochloride UNII-0FC27E442O GSK2110183 Afuresertib (hydrochloride) |
| Description | Afuresertib hydrochloride is a potent and ATP-competitive specific Akt inhibitor. |
|---|---|
| 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℃ |