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GLPG0634 analog

🥰Excellent
Catalog No. T3076Cas No. 1206101-20-3
Alias 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

GLPG0634 analog

🥰Excellent
Purity: 100%
Catalog No. T3076Alias GLPG0634 analogueCas No. 1206101-20-3
GLPG0634 analog (GLPG0634 analogue) is a specific JAK1 inhibitor with IC50 of 10/28/810/116 nM for JAK1/2/3 and TYK2, respectively.
Pack SizePriceAvailabilityQuantity
1 mg$34In Stock
2 mg$48In Stock
5 mg$80In Stock
10 mg$147In Stock
25 mg$277In Stock
50 mg$490In Stock
100 mg$693In Stock
500 mg$1,450In Stock
1 mL x 10 mM (in DMSO)$89In Stock
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Purity:100%
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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, JAK1:10nM, JAK2:28nM, 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].
AliasGLPG0634 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.
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

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TargetMol | Animal experimentsFor example, your dosage is 10 mg/kg Each animal weighs 20 g, and the dosage volume is 100 μL . TargetMol | Animal experiments A total of 10 animals were administered, and the formula you used is 5% TargetMol | reagent DMSO+30% PEG300+5% Tween 80+60% ddH2O. So your working solution concentration is 2 mg/mL。
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Preparation method for in vivo formula: Take 50 μL DMSOTargetMol | reagent main solution, add 300 μLPEG300TargetMol | reagent mix well and clarify, then add 50 more μL Tween 80, mix well and clarify, then add 600 more μLddH2OTargetMol | reagent mix well and clarify
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