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AT13148

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Catalog No. T2482Cas No. 1056901-62-2

AT13148 is an oral-active and ATP-competitive, multi-AGC kinase inhibitor for Akt1/2/3, p70S6K, PKA, and ROCKI/II.

AT13148

AT13148

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Purity: 99.65%
Catalog No. T2482Cas No. 1056901-62-2
AT13148 is an oral-active and ATP-competitive, multi-AGC kinase inhibitor for Akt1/2/3, p70S6K, PKA, and ROCKI/II.
Pack SizePriceUSA WarehouseGlobal WarehouseQuantity
1 mg$30In StockIn Stock
5 mg$89In StockIn Stock
10 mg$139In StockIn Stock
25 mg$247In StockIn Stock
50 mg$396In StockIn Stock
1 mL x 10 mM (in DMSO)$98In StockIn 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:99.65%
Color:White
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Product Introduction

Bioactivity
Description
AT13148 is an oral-active and ATP-competitive, multi-AGC kinase inhibitor for Akt1/2/3, p70S6K, PKA, and ROCKI/II.
Targets&IC50
SGK3:63 nM, Akt1:38 nM, ROCK2:4 nM, RSK1:85 nM, p70 S6K:8 nM, Akt2:402 nM, Chk2:860 nM, PKA:3 nM, ROCK1:6 nM, Aurora B:1840 nM, Akt3:50 nM
In vitro
In PTEN-deficient MES-SA cells, AT13148 was able to inhibit AKT and p70S6K signaling. In cancer cell lines with aberrant PI3K-AKT-mTOR or RAS-RAF pathways (GI50=1.5-3.8 μM), AT13148 was able to inhibit multiple AGC kinases, thereby suppressing cancer cell proliferation.
In vivo
In PTEN-deficient MES-SA cells, AT13148 was able to inhibit AKT and p70S6K signaling. In cancer cell lines with aberrant PI3K-AKT-mTOR or RAS-RAF pathways (GI50=1.5-3.8 μM), AT13148 was able to inhibit multiple AGC kinases, thereby suppressing cancer cell proliferation.
Kinase Assay
In vitro kinase assays: AT13148 is assayed against 40 kinases and the percentage inhibition at 10 μM of AT13148 is determined. Individual IC50 values are measured for selected kinases using ATP concentrations equivalent to the Km for each enzyme.
Cell Research
Cytotoxicity is determined using a 72 h Alamar Blue assay or a 96 h SRB assay. (Only for Reference)
Chemical Properties
Molecular Weight313.78
FormulaC17H16ClN3O
Cas No.1056901-62-2
SmilesNC[C@@](O)(c1ccc(Cl)cc1)c1ccc(cc1)-c1cn[nH]c1
Relative Density.1.328 g/cm3 (Predicted)
Storage & Solubility Information
Storagestore at low temperature | Powder: -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 (insoluble or slightly soluble)
DMSO: 58 mg/mL (184.84 mM), Sonication is recommended.
In Vivo Formulation
10% DMSO+40% PEG300+5% Tween 80+45% Saline: 2 mg/mL (6.37 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
DMSO
1mg5mg10mg50mg
1 mM3.1869 mL15.9347 mL31.8695 mL159.3473 mL
5 mM0.6374 mL3.1869 mL6.3739 mL31.8695 mL
10 mM0.3187 mL1.5935 mL3.1869 mL15.9347 mL
20 mM0.1593 mL0.7967 mL1.5935 mL7.9674 mL
50 mM0.0637 mL0.3187 mL0.6374 mL3.1869 mL
100 mM0.0319 mL0.1593 mL0.3187 mL1.5935 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:
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2 Enter the in vivo formulation:
% DMSO
%
% Tween 80
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Dose Conversion

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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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