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Afuresertib
🥰Excellent
Catalog No. T1911Cas No. 1047644-62-1
Alias GSK2110183C, GSK2110183
Afuresertib (GSK2110183) is an orally bioavailable inhibitor of the serine/threonine protein kinase Akt (protein kinase B) with potential antineoplastic activity.
Afuresertib
🥰Excellent
Purity: 99.17%
Catalog No. T1911Alias GSK2110183C, GSK2110183Cas No. 1047644-62-1
Afuresertib (GSK2110183) is an orally bioavailable inhibitor of the serine/threonine protein kinase Akt (protein kinase B) with potential antineoplastic activity.
| 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 |
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Purity:99.17%
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All TargetMol products are for research purposes only and cannot be used for human consumption. We do not provide products or services to individuals. Please comply with the intended use and do not use TargetMol products for any other purpose.Product Introduction
Bioactivity
Chemical Properties
| Description | Afuresertib (GSK2110183) is an orally bioavailable inhibitor of the serine/threonine protein kinase Akt (protein kinase B) with potential antineoplastic activity. |
| Targets&IC50 | Akt3:2.6 nM(Ki), Akt1:0.08 nM(Ki), Akt2:2 nM(Ki) |
| In vitro | Overall 65% of hematological cell lines were sensitive to Afuresertib with an EC50 < 1 μM. 21% of solid tumor cell lines tested had an EC50 < 1 μM for Afuresertib. Afuresertib inhibited the kinase activity of the E17K AKT1 mutant protein with an EC50 of 0.2 nM. Afuresertib showed Afuresertib showed a concentration-dependent effect on the phosphorylation levels of multiple AKT substrates, including GSK3b, PRAS40, FOXO and cystatin 9. |
| In vivo | Overall 65% of hematological cell lines were sensitive to Afuresertib with an EC50 < 1 μM. 21% of solid tumor cell lines tested had an EC50 < 1 μM for Afuresertib. Afuresertib inhibited the kinase activity of the E17K AKT1 mutant protein with an EC50 of 0.2 nM. Afuresertib showed Afuresertib showed a concentration-dependent effect on the phosphorylation levels of multiple AKT substrates, including GSK3b, PRAS40, FOXO and cystatin 9. |
| 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 |
| Smiles | Cn1ncc(Cl)c1-c1cc(sc1Cl)C(=O)N[C@H](CN)Cc1cccc(F)c1 |
| Relative Density. | 1.49 g/cm3 (Predicted) |
Storage & Solubility Information
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | |||||||||||||||||||||||||||||||||||
| Solubility Information | DMSO: 50 mg/mL (117.01 mM)  Ethanol: 79 mg/mL (184.9 mM) | |||||||||||||||||||||||||||||||||||
Solution Preparation Table | ||||||||||||||||||||||||||||||||||||
DMSO/Ethanol
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In Vivo Formulation Calculator (Clear solution)
Please enter your animal experiment information in the following box and click Calculate to obtain the mother liquor preparation method and in vivo formula preparation method:
For example, your dosage is 10 mg/kg Each animal weighs 20 g, and the dosage volume is 100 μL . A total of 10 animals were administered, and the formula you used is 5% 
DMSO+30% PEG300+5% Tween 80+60% ddH2O. So your working solution concentration is 2 mg/mL。Mother liquor preparation method: 2 mg of drug dissolved in 50 μL DMSO (mother liquor concentration of 40 mg/mL), if you need to configure a concentration that exceeds the solubility of the product, please contact us first.
(mother liquor concentration of 40 mg/mL), if you need to configure a concentration that exceeds the solubility of the product, please contact us first.Preparation method for in vivo formula: Take 50 μL DMSO main solution, add 300 μLPEG300 mix well and clarify, then add 50 more μL Tween 80, mix well and clarify, then add 600 more μLddH2O mix well and clarify
main solution, add 300 μLPEG300 mix well and clarify, then add 50 more μL Tween 80, mix well and clarify, then add 600 more μLddH2O mix well and clarifyFor Reference Only. Please develop an appropriate dissolution method based on your laboratory animals and route of administration.
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