GLPG0634 analogue

Catalog No.S7137

GLPG0634 analogue Chemical Structure

Molecular Weight(MW): 410.43

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.

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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 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 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]

Protocol

Animal Research:

[1]

+ Expand
  • Animal Models: Rat CIA model and mouse CIA model
  • Formulation: 0.5% (v/v) methylcellulose
  • Dosages: 30 mg/kg daily (Rats); 50 mg/kg twice daily (Mice)
  • Administration: p.o.
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 0.1 mg/mL (0.24 mM)
Water Insoluble
Ethanol Insoluble

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 410.43
Formula

C23H18N6O2

CAS No. 1206101-20-3
Storage powder
Synonyms N/A

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Clinical Trial Information

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT02162355 Completed Healthy Galapagos NV June 2014 Phase 1
NCT02084199 Completed Renal Impairment Galapagos NV March 2014 Phase 1
NCT02048618 Completed Crohns Disease Galapagos NV February 2014 Phase 2
NCT01915667 Completed Healthy Galapagos NV July 2013 Phase 1
NCT01894516 Completed Rheumatoid Arthritis Galapagos NV July 2013 Phase 2
NCT01888874 Completed Rheumatoid Arthritis Galapagos NV July 2013 Phase 2

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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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JAK Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID