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AT7867 as a novel and potent inhibitor of both AKT and the downstream kinase p70 S6 kinase (p70S6K) and also of protein kinase A. This ATP-competitive small molecule potently inhibits both AKT and p70S6K activity at the cellular level, as measured by inhibition of GSK3β and S6 ribosomal protein phosphorylation, and also causes growth inhibition in a range of human cancer cell lines as a single agent.
| Cell Experiment | |
|---|---|
| Cell lines | PTEN-negative U87MG human glioblastoma cells |
| Preparation method | Alamar Blue Cell Proliferation Assay. Cells were plated in 96-well microplates at 5000 cells per well in medium supplemented with 10% FBS, and grown for 24 hours before treatment with AT7867. Inhibitor or vehicle control was added to the cells for 72 hours. Following this, Alamar Blue solution (BioSource, Nivelle Belgium) was added as stated in the manufacturer's instructions. The IC50 value for each inhibitor was calculated in GraphPad Prism (San Diego, USA) using non-linear regression analysis and a sigmoidal dose-response (variable slope) equation. |
| Concentrations | 0~100 μM |
| Incubation time | 72 h |
| Animal Experiment | |
|---|---|
| Animal models | athymic BALB/c mice bearing MES-SA and U87MG human glioblastoma xenograft tumors |
| Formulation | 10% DMSO, 90% saline |
| Dosages | 20mg/kg or 90mg/kg once every 3 days |
| Administration | p.o. |
| Molecular Weight | 337.85 |
| Formula | C20H20ClN3 |
| CAS Number | 857531-00-1 |
| Solubility (25°C) | DMSO 60 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| Related Akt Products |
|---|
| GSK690693
GSK690693 is a potent Akt inhibitor (Akt1 IC50 = 2 nM, Akt2 IC50 = 13 nM, Akt3 IC50 = 9 nM) which also inhibited the phosphorylation of the downstream target GSK3b in cells. |
| Perifosine
Perifosine is an orally active Akt inhibitor, the antiproliferative properties of Perifosine with an IC50 of 0.6–8.9 µM. |
| MK-2206 2HCl
MK-2206 is a novel allosteric inhibitor of Akt with IC50 values of 8 nM, 12 nM and 65 nM for Akt1, Akt2 and Akt3, respectively. |
| Ipatasertib
Ipatasertib (GDC-0068, RG7440) is a potent and selective, ATP-competitive Akt inhibitor with IC50 values of 5 to 18 nM. |
| Triciribine
Triciribine (API-2, NSC 154020) is a selective inhibitor of Akt (protein kinase B) signaling with IC50 of 130 nM. |
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