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A66

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Catalog No. T2418Cas No. 1166227-08-2

A66 is a specific and effective p110α inhibitor(IC50=32 nM).

A66

A66

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Purity: 99.51%
Catalog No. T2418Cas No. 1166227-08-2
A66 is a specific and effective p110α inhibitor(IC50=32 nM).
Pack SizePriceUSA WarehouseGlobal WarehouseQuantity
2 mg$30In StockIn Stock
5 mg$46In StockIn Stock
10 mg$76In StockIn Stock
25 mg$147In StockIn Stock
50 mg$259In StockIn Stock
100 mg$383In StockIn Stock
200 mg$538In StockIn Stock
1 mL x 10 mM (in DMSO)$51In StockIn Stock
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In Stock Estimated shipping dateUSA Warehouse[1-2 days] Global Warehouse[5-7 days]
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Purity:99.51%
Color:White
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Product Introduction

Bioactivity
Description
A66 is a specific and effective p110α inhibitor(IC50=32 nM).
Targets&IC50
p110α-E545K:30 nM, p110α-H1047R:43 nM, p110γ:3480 nM, p110α:32 nM, PI4Kβ:236 nM, PI3KC2β:462 nM
In vitro
In male CD1 mice, A66 (10 mg/kg) increased glucose production during the pyruvate tolerance test. In SK-OV-3 tumor tissues, A66 (100 mg/kg) effectively reduced the phosphorylation of Akt/PKB and p70 S6 kinase, inhibiting tumor cell growth.
In vivo
A66 significantly inhibits the oncogenic forms of p110α, such as p110αE545K (IC50=30 nM) and p110αH1047R (IC50=43 nM), effectively reducing their activity.
Kinase Assay
IC50 values are evaluated using the PI3K (human) HTRF Assay. p85α/p110δ is obtained from Invitrogen. All other isoforms are produced in-house by co-expressing full-length human p85α with the indicated human full-length catalytic subunit containing a histidine tag at the N-terminus to allow purification. The PI3Ks are titrated and used at a concentration between their EC65-EC80 values. PI3K activity in immunoprecipitates is assayed using an antibody to the N-SH2 (N-Src homology 2) domain of p85α. Assays for other lipid kinases and protein kinases are performed by the National Centre for Protein Kinase Profiling and Invitrogen Drug Discovery Services[1].
Chemical Properties
Molecular Weight393.53
FormulaC17H23N5O2S2
Cas No.1166227-08-2
SmilesCc1nc(NC(=O)N2CCC[C@H]2C(N)=O)sc1-c1csc(n1)C(C)(C)C
Relative Density.1.354 g/cm3
Storage & Solubility Information
StoragePowder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
Solubility Information
H2O: < 1 mg/mL (insoluble or slightly soluble)
Ethanol: 1 mg/mL (2.54 mM), Sonication is recommended.
DMSO: 60 mg/mL (152.47 mM), Sonication is recommended.
In Vivo Formulation
10% DMSO+40% PEG300+5% Tween 80+45% Saline: 2 mg/mL (5.08 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
1mg5mg10mg50mg
1 mM2.5411 mL12.7055 mL25.4110 mL127.0551 mL
DMSO
1mg5mg10mg50mg
5 mM0.5082 mL2.5411 mL5.0822 mL25.4110 mL
10 mM0.2541 mL1.2706 mL2.5411 mL12.7055 mL
20 mM0.1271 mL0.6353 mL1.2706 mL6.3528 mL
50 mM0.0508 mL0.2541 mL0.5082 mL2.5411 mL
100 mM0.0254 mL0.1271 mL0.2541 mL1.2706 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:
TargetMol | Animal experiments 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 DMSOTargetMol | 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 DMSOTargetMol | reagent stock solution to 400 μL PEG300TargetMol | reagent 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 ddH2OTargetMol | 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.
1 Enter information below:
mg/kg
g
μL
2 Enter the in vivo formulation:
% DMSO
%
% Tween 80
% Saline/PBS/ddH2O

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

Keywords

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