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Pack Size | Price | Availability | Quantity |
---|---|---|---|
1 mg | $33 | In Stock | |
2 mg | $46 | In Stock | |
5 mg | $72 | In Stock | |
10 mg | $98 | In Stock | |
25 mg | $178 | In Stock | |
50 mg | $288 | In Stock | |
100 mg | $503 | In Stock | |
500 mg | $1,090 | In Stock | |
1 mL x 10 mM (in DMSO) | $72 | In Stock |
Description | Afuresertib (GSK2110183) is an orally bioavailable inhibitor of the serine/threonine protein kinase Akt (protein kinase B) with potential antineoplastic activity. |
Kinase Assay | Potency (Ki*) of afuresertib: The true potency (Ki*) of the inhibitor is initially determined at low enzyme concentrations (0.1 nM AKT1, 0.7 nM AKT2, and 0.2 nM AKT3) using a filter binding assay and then confirmed with progress curve analysis. In the filter binding assay, a pre-mix of enzyme plus inhibitor is incubated for 1 h and then added to a GSKα peptide (Ac-KKGGRARTSS-FAEPG-amide) and [γ33P] ATP. Reactions are terminated after 2 h and the radio labeled AKT peptide product is captured in a phospho-cellulose filter plate. Progress curve analysis utilizes continuous real-time fluorescence detection of product formation using the Sox-AKT-tide substrate (Ac-ARKRERAYSF-d-Pro-Sox-Gly-NH2). |
Cell Research | A 3-day proliferation assay using CellTiter-Glo is performed to measure the growth inhibition by the compounds at 0-30 μM. Cell growth is determined relative to untreated (DMSO) controls. EC50's are calculated from inhibition curves using a 4- or 6-parameter fitting algorithm in the Assay Client application.(Only for Reference) |
Alias | GSK2110183C, GSK2110183 |
Molecular Weight | 427.32 |
Formula | C18H17Cl2FN4OS |
Cas No. | 1047644-62-1 |
Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | |||||||||||||||||||||||||||||||||||
Solubility Information | DMSO: 50 mg/mL (117.01 mM) ![]() Ethanol: 79 mg/mL (184.9 mM) | |||||||||||||||||||||||||||||||||||
Solution Preparation Table | ||||||||||||||||||||||||||||||||||||
Ethanol/DMSO
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