1047644-62-1
1047644-62-1 structure
- Name: afuresertib
- Chemical Name: gsk-2110183
- CAS Number: 1047644-62-1
- Molecular Formula: C18H17Cl2FN4OS
- Molecular Weight: 427.32300
- Catalog: Biochemical Inhibitor PI3K/Akt/mTOR inhibitor (PI3K/Akt/mTOR) Akt inhibitor
- Create Date: 2018-03-19 07:50:23
- Modify Date: 2024-01-10 23:16:52
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Afuresertib is a potent and ATP-competitive specific Akt inhibitor.
| Name | gsk-2110183 |
|---|---|
| Synonyms |
N-[1(S)-2-amino-(3-fluorobenzyl)ethyl]-5-chloro-4-(4-chloro-1-methyl-1H-pyrazol-5-yl)thiophene-2-carboxamide
N-{(1S)-2-amino-1-[(3-fluorophenyl)methyl] ethyl}-5-chloro-4-(4-chloro-1-methyl-1H-pyrazol-5-yl)-2-thiophenecarboxamide N-{(1S)-2-amino-1-[(3-fluorophenyl)methyl]ethyl}-5-chloro-4-(4-chloro-1-methyl-1H-pyrazol-5-yl)-2-thiophenecarboxamide afuresertib |
| Description | Afuresertib 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 | C18H17Cl2FN4OS |
|---|---|
| Molecular Weight | 427.32300 |
| Exact Mass | 426.04800 |
| PSA | 101.18000 |
| LogP | 4.98550 |
| Storage condition | -20℃ |