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Afuresertib

Name: Afuresertib
Brand: TargetMol
SKU: T1911
Price: 33 USD
Availability: InStock
Rating: 5 (10 reviews)

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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

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Purity: 99.51%

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	USA Warehouse	Global Warehouse
1 mg	$33	In Stock	In Stock
2 mg	$46	In Stock	In Stock
5 mg	$72	In Stock	In Stock
10 mg	$98	In Stock	In Stock
25 mg	$178	In Stock	In Stock
50 mg	$288	In Stock	In Stock
100 mg	$503	In Stock	In Stock
500 mg	$1,090	-	In Stock
1 mL x 10 mM (in DMSO)	$72	In Stock	In Stock

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In Stock Estimated shipping dateUSA Warehouse[1-2 days] Global Warehouse[5-7 days]

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.

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Purity:99.51%

Color:White to Yellow

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COA HNMR LCMS

Product Introduction

Bioactivity

Description	Afuresertib (GSK2110183) is an orally bioavailable inhibitor of the serine/threonine protein kinase Akt (protein kinase B) with potential antineoplastic activity.
Targets&IC50	Akt2:2 nM(Ki), Akt1:0.08 nM(Ki), Akt3:2.6 nM(Ki), ROCK:100 nM, PKCη:210 nM, PKCθ:510 nM, PKCβI:430 nM
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)
Synonyms	GSK2110183C, GSK2110183

Chemical Properties

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

In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.

Solubility Information

DMSO: 250 mg/mL (585.04 mM), Sonication is recommended.

Ethanol: 79 mg/mL (184.87 mM), Sonication is recommended.

In Vivo Formulation

10% DMSO+40% PEG300+5% Tween 80+45% Saline: 2 mg/mL (4.68 mM), Sonication is recommended.

Please add the solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately. The formulation provided above is for reference purposes only. In vivo formulations may vary and should be modified based on specific experimental conditions.

Solution Preparation Table

Ethanol/DMSO

	1mg	5mg	10mg	50mg
1 mM	2.3402 mL	11.7008 mL	23.4017 mL	117.0083 mL
5 mM	0.4680 mL	2.3402 mL	4.6803 mL	23.4017 mL
10 mM	0.2340 mL	1.1701 mL	2.3402 mL	11.7008 mL
20 mM	0.1170 mL	0.5850 mL	1.1701 mL	5.8504 mL
50 mM	0.0468 mL	0.2340 mL	0.4680 mL	2.3402 mL
100 mM	0.0234 mL	0.1170 mL	0.2340 mL	1.1701 mL

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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 stock solution preparation method and in vivo formula preparation method:

For example, if the intended dosage is 10 mg/kg for animals weighing 20 g , with a dosing volume of 100 μL per animal, TargetMol | Animal experiments

and a total of 10 animals are to be administered, using a formulation of TargetMol | reagent

10% DMSO+ 40% PEG300+ 5% Tween 80+ 45% Saline/PBS/ddH₂O , the resulting working solution concentration would be 2 mg/mL.

Stock Solution Preparation:

Dissolve 2 mg of the compound in 100 μL DMSO TargetMol | reagent to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.

Preparation of the In Vivo Formulation:

1) Add 100 μL of the DMSO TargetMol | reagent stock solution to 400 μL PEG300 and mix thoroughly until the solution becomes clear.

2) Add 50 μL Tween 80 and mix well until fully clarified.

3) Add 450 μL Saline,PBS or ddH₂O TargetMol | reagent and mix thoroughly until a homogeneous solution is obtained.

This example is provided solely to demonstrate the use of the In Vivo Formulation Calculator and does not constitute a recommended formulation for any specific compound. Please select an appropriate dissolution and formulation strategy based on your experimental model and route of administration.

All co-solvents required for this protocol, includingDMSO, PEG300/PEG400, Tween 80, SBE-β-CD, and Corn oil, are available for purchase on the TargetMol website.

Dose Conversion

You can also refer to dose conversion for different animals. More Dose Conversion

Tech Support

Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc