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Afuresertib hydrochloride (GSK 2110183 hydrochloride) is an orally bioavailable, selective, ATP-competitive and potent pan-Akt kinase inhibitor with Kis of 0.08/2/2.6 nM for Akt1/Akt2/Akt3 respectively. Afuresertib HCl binds to and inhibits the activity of Akt, which may result in inhibition of the PI3K/Akt signaling pathway and tumor cell proliferation and the induction of tumor cell apoptosis. 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. Afuresertib significantly enhances cisplatin-induced cytotoxicity. Afuresertib modulates the expression E2F1 and MYC, which are associated with fibroblast core serum response.
| Cell Experiment | |
|---|---|
| Cell lines | MPM cells |
| Preparation method | 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. |
| Concentrations | 50, 20, 10, 5, 2, 1, 0.5, 0.2, 0.1, and 0.01 μM |
| Incubation time | 72 h |
| Animal Experiment | |
|---|---|
| Animal models | |
| Formulation | |
| Dosages | |
| Administration | |
| Molecular Weight | 463.78 |
| Formula | C18H18Cl3FN4OS |
| CAS Number | 1047645-82-8 |
| Solubility (25°C) | DMSO 90 mg/mL |
| Storage | -20°C, protect from light, sealed |
| Related Akt Products |
|---|
| (E)-Akt inhibitor-IV
(E)-Akt inhibitor-IV is a PI3K-Akt inhibitor, with potent cytotoxic. |
| K-80003
K-80003 is a potent inhibitor of tRXRα-dependent Akt activation and cancer cell growth. |
| FPA-124
FPA-124, a cell-permeable copper complex, is a selective Akt inhibitor with an IC50 of 0.1 μM. |
| SPOP-IN-1
SPOP-IN-1 is a selective SPOP E3 ubiquitin ligase inhibitor. |
| 10-DEBC hydrochloride
10-DEBC hydrochloride is a selective Akt inhibitor, with an IC50 of 1.28 μM. |
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