Home JAK/STAT JAK inhibitor GLPG0634 analogue For research use only.

GLPG0634 analogue

GLPG0634 analogue is a selective JAK1 inhibitor with IC50 of 10 nM, 28 nM, 810 nM, and 116 nM for JAK1, JAK2, JAK3, and TYK2, respectively. Phase 2.

GLPG0634 analogue Chemical Structure

GLPG0634 analogue Chemical Structure

CAS No. 1206101-20-3

Purity & Quality Control

GLPG0634 analogue Related Products

Signaling Pathway

JAK Signaling Pathways

JAK Signaling Pathway

Biological Activity

Description GLPG0634 analogue is a selective JAK1 inhibitor with IC50 of 10 nM, 28 nM, 810 nM, and 116 nM for JAK1, JAK2, JAK3, and TYK2, respectively. Phase 2.
Targets
JAK [1]
In vitro
In vitro In cell lines, GLPG0634 inhibits IL-2- and IL-4-induced JAK1/JAK3/γc signaling and IFN-αB2-induced JAK1/TYK2 type II receptor signaling with IC50 ranged from 150 to 760 nM. GLPG0634 shows higher selectivity for JAK/STAT signaling involving JAK1 than JAK2 kinase in a cellular context. Besides, GLPG0634 also inhibits the differentiation of Th1, Th2, and Th17 cells. [1]
In Vivo
In vivo Following oral administration, the absolute bioavailability was moderate in rats (45%) and high in mice (∼100%). GLPG0634 (30 mg/kg daily (Rats); 50 mg/kg twice daily (Mice)) dose-dependently reduces inflammation, cartilage, and bone degradation in the CIA model in rats and mice. [1]
Animal Research Animal Models Rat CIA model and mouse CIA model
Dosages 30 mg/kg daily (Rats); 50 mg/kg twice daily (Mice)
Administration p.o.
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT02048618 Completed
Crohn''s Disease
Galapagos NV
 February 2014 Phase 2
NCT01820806 Completed
Healthy
Galapagos NV
 March 2013 Phase 1
NCT01798979 Completed
Healthy
Galapagos NV
 February 2013 Phase 1
NCT01665924 Completed
Healthy
Galapagos NV
 July 2012 Phase 1

Chemical Information & Solubility

Molecular Weight 410.43 Formula

C23H18N6O2
CAS No. 1206101-20-3 SDF Download GLPG0634 analogue SDF
Smiles C1CC1C(=O)NC2=NN3C(=N2)C=CC=C3C4=CC=C(C=C4)CN5CCS(=O)(=O)CC5
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 82 mg/mL ( (199.79 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : Insoluble

Ethanol : Insoluble


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In vivo
Batch:

Add solvents to the product individually and in order.


In vivo Formulation Calculator

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In vivo Formulation Calculator (Clear solution)

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Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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