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SGC-GAK-1

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Catalog No. T5169Cas No. 2226517-76-4

SGC-GAK-1 is a selective cyclin G-associated kinase (GAK) inhibitor (Ki: 3.1 nM).

SGC-GAK-1

SGC-GAK-1

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Purity: 99.85%
Catalog No. T5169Cas No. 2226517-76-4
SGC-GAK-1 is a selective cyclin G-associated kinase (GAK) inhibitor (Ki: 3.1 nM).
Pack SizePriceUSA WarehouseGlobal WarehouseQuantity
5 mg$43In StockIn Stock
10 mg$73In StockIn Stock
25 mg$148In StockIn Stock
50 mg$238In StockIn Stock
100 mg$353In StockIn Stock
200 mg$493-In Stock
1 mL x 10 mM (in DMSO)$47In 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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Batch Information

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Purity:99.85%
Appearance:Solid
Color:Yellow
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Product Introduction

Bioactivity
Description
SGC-GAK-1 is a selective cyclin G-associated kinase (GAK) inhibitor (Ki: 3.1 nM).
Targets&IC50
GAK:3.1 nM (Ki)
In vitro
SGC-GAK-1 potently binds GAK (Ki: 3.1 nM; Kd: 1.9 nM). SGC-GAK-1 showed strong growth inhibition in LNCaP, VCaP, and 22Rv1 cells at 10 μM, but the minimal effect in PC3 and DU145 cells. In dose-response SGC-GAK-1 showed potent antiproliferative activity in LNCaP and 22Rv1 cells at a similar dose range that it engages GAK.
Chemical Properties
Molecular Weight389.24
FormulaC18H17BrN2O3
Cas No.2226517-76-4
SmilesCOc1cc(Nc2ccnc3ccc(Br)cc23)cc(OC)c1OC
Relative Density.1.436 g/cm3 (Predicted)
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
Ethanol: 15 mg/mL (38.54 mM), Sonication is recommended.
DMSO: 55 mg/mL (141.3 mM), Sonication is recommended.
In Vivo Formulation
10% DMSO+40% PEG300+5% Tween 80+45% Saline: 2 mg/mL (5.14 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 mM2.5691 mL12.8455 mL25.6911 mL128.4555 mL
5 mM0.5138 mL2.5691 mL5.1382 mL25.6911 mL
10 mM0.2569 mL1.2846 mL2.5691 mL12.8455 mL
20 mM0.1285 mL0.6423 mL1.2846 mL6.4228 mL
DMSO
1mg5mg10mg50mg
50 mM0.0514 mL0.2569 mL0.5138 mL2.5691 mL
100 mM0.0257 mL0.1285 mL0.2569 mL1.2846 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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