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GLPG0634 analogue JAK inhibitor

Cat.No.S7137

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 JAK inhibitor Chemical Structure

Chemical Structure

Molecular Weight: 410.43

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Quality Control

Batch: Purity: 99.80%
99.80

Solubility

In vitro
Batch:

DMSO : 82 mg/mL (199.79 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Water : Insoluble

Ethanol : Insoluble

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In vivo
Batch:

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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.
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Chemical Information, Storage & Stability

Molecular Weight 410.43 Formula

C23H18N6O2

 Storage (From the date of receipt)
CAS No. 1206101-20-3 Download SDF Storage of Stock Solutions

Synonyms N/A Smiles C1CC1C(=O)NC2=NN3C(=N2)C=CC=C3C4=CC=C(C=C4)CN5CCS(=O)(=O)CC5

Mechanism of Action

Targets/IC50/Ki
JAK
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.
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.
References

Clinical Trial Information

(data from https://clinicaltrials.gov, updated on 2024-05-22)

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

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