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GLPG0634 analog (Synonyms: GLPG0634 analogue)

Catalog No. T3076 Copy Product Info
Purity: 99.64%
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GLPG0634 analog (GLPG0634 analogue) is a specific JAK1 inhibitor with IC50 of 10/28/810/116 nM for JAK1/2/3 and TYK2, respectively.

GLPG0634 analog

Copy Product Info
🥰Excellent
Catalog No. T3076
Synonyms GLPG0634 analogue

GLPG0634 analog (GLPG0634 analogue) is a specific JAK1 inhibitor with IC50 of 10/28/810/116 nM for JAK1/2/3 and TYK2, respectively.

GLPG0634 analog
Cas No. 1206101-20-3
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Pack SizePriceUSA StockGlobal StockQuantity
1 mg$34In StockIn Stock
2 mg$48In StockIn Stock
5 mg$80In StockIn Stock
10 mg$147In StockIn Stock
25 mg$277In StockIn Stock
50 mg$490In StockIn Stock
100 mg$693In StockIn Stock
500 mg$1,450-In Stock
1 mL x 10 mM (in DMSO)$89In StockIn Stock
For In stock only · Estimated delivery: USA Stock (1-2 days) Global Stock (5-7 days)
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For research use only—not for human use. No sales to individuals. Use as intended only.
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Purity:99.64%
Color:White
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Product Introduction

Bioactivity
Description
GLPG0634 analog (GLPG0634 analogue) is a specific JAK1 inhibitor with IC50 of 10/28/810/116 nM for JAK1/2/3 and TYK2, respectively.
Targets&IC50
JAK3:810nM, JAK2:28nM, JAK1:10nM, TYK2:116 nM
In vitro
In multiple cell lines, GLPG0634 inhibited IFN-αB2-induced JAK1/TYK2 type II receptor signaling and IL-2/4-induced JAK1/JAK3/γc signaling (IC50: 150-760 nM). At the cellular level, GLPG0634 was more selective for JAK1-containing JAK/STAT signaling than JAK2 kinase. In addition, GLPG0634 inhibited the proliferation of Th1/Th2/Th17 cells.
In vivo
In multiple cell lines, GLPG0634 inhibited IFN-αB2-induced JAK1/TYK2 type II receptor signaling and IL-2/4-induced JAK1/JAK3/γc signaling (IC50: 150-760 nM). At the cellular level, GLPG0634 was more selective for JAK1-containing JAK/STAT signaling than JAK2 kinase. In addition, GLPG0634 inhibited the proliferation of Th1/Th2/Th17 cells.
Kinase Assay
EC50 values of the test compounds are calculated from serial dilution series ranging from 200 to 0.1 μM. Cells are seeded in 96-well plates at a density of 5,000 cells per well in 100 μL medium. The next day, 100 μL medium containing each test compound is added. Cells are incubated for 16 h, fixed and processed for automated microscopy. EC50 estimates are calculated using four-parameter log-logistic fit with the package drc[1].
SynonymsGLPG0634 analogue
Chemical Properties
Molecular Weight410.43
FormulaC23H18N6O2
Cas No.1206101-20-3
SmilesO=C(Nc1nc2cccc(-c3ccc(OCc4ccc(nc4)C#N)cc3)n2n1)C1CC1
Relative Density.no data available
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
DMSO: 7.5 mg/mL (18.27 mM), Sonication is recommended.
Solution Preparation Table
DMSO
1mg5mg10mg50mg
1 mM2.4365 mL12.1823 mL24.3647 mL121.8235 mL
5 mM0.4873 mL2.4365 mL4.8729 mL24.3647 mL
10 mM0.2436 mL1.2182 mL2.4365 mL12.1823 mL
Note : The dilution table applies only to solid products. For liquid products, please calculate the stock solution based on the stated concentration and/or density.

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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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