Filgotinib (GLPG0634)

Catalog No.S7605 Batch:S760503

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Technical Data

Formula

C21H23N5O3S
Molecular Weight 425.50 CAS No. 1206161-97-8
Solubility (25°C)* In vitro DMSO 21 mg/mL (49.35 mM)
Water Insoluble
Ethanol Insoluble
In vivo (Add solvents to the product individually and in order)
Clear solution
4%DMSO 30%PEG300 66%ddH2O
3.0mg/ml Taking the 1 mL working solution as an example, add 40 μL of 75 mg/ml clarified DMSO stock solution to 300 μL of PEG 300, mix evenly to clarify it; then continue to add 660 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results. 
* <1 mg/ml means slightly soluble or 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.
* Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

Preparing Stock Solutions

Biological Activity

Description Filgotinib (GLPG0634) 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
JAK1 [1]
(Cell-free assay)		 JAK2 [1]
(Cell-free assay)		 TYK2 [1]
(Cell-free assay)		 JAK3 [1]
(Cell-free assay)
10 nM 28 nM 116 nM 810 nM
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 is moderate in rats (45%) and high in mice (∼100%). Filgotinib (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] Filgotinib (GLPG0634) in DSS-treated mice demonstrates that inhibition of JAK1 is sufficient for achieving strong efficacy in pre-clinical mouse model, correlated to the inhibition of STAT3 phosphorylation in the inflamed colon. [2]

Protocol (from reference)

Animal Study:[1]
  • Animal Models

    Rat CIA model and mouse CIA model

  • Dosages

    30 mg/kg daily (Rats); 50 mg/kg twice daily (Mice)

  • Administration

    p.o.

Customer Product Validation

Data from [Data independently produced by , , Arthritis Rheumatol, 2018, 70(12):2057-2066]

Data from [Data independently produced by , , Mol Cell Endocrinol, 2018, 472:26-39]

Selleck's Filgotinib (GLPG0634) has been cited by 45 publications

Effect of JAK inhibitors on the three forms of bone damage in autoimmune arthritis: joint erosion, periarticular osteopenia, and systemic bone loss [ Inflamm Regen, 2023, 43(1):44] PubMed: 37726797
JAK inhibitors differentially modulate B cell activation, maturation and function: A comparative analysis of five JAK inhibitors in an in-vitro B cell differentiation model and in patients with rheumatoid arthritis [ Front Immunol, 2023, 14:1087986] PubMed: 36776828
Sustained induction of IP-10 by MRP8/14 via the IFNβ-IRF7 axis in macrophages exaggerates lung injury in endotoxemic mice [ Burns Trauma, 2023, 11:tkad006] PubMed: 37701855
The protective effect of leukemia inhibitory factor on apoptosis of BMSCs induced by hypoxia and serum-deprivation [ Am J Transl Res, 2023, 15(6):4065-4078] PubMed: 37434853
Effect of JAK inhibitors on the three forms of bone damage in autoimmune arthritis: joint erosion, periarticular osteopenia, and systemic bone loss [ Inflamm Regen, 2023, 43(1):44] PubMed: 37726797
Effects of Indole Derivative IDC16 on Cell Proliferation, Transfection, and Alternative Splicing in Production of Lentiviral Vectors by Transient Co-Transfection [ DigitalCommons, 2023, 10.26076/aa7d-bd6d] PubMed: none
Tyrosine phosphorylation regulates RIPK1 activity to limit cell death and inflammation [ Nat Commun, 2022, 13(1):6603] PubMed: 36329033
Oncogenic TYK2P760L kinase is effectively targeted by combinatorial TYK2, mTOR and CDK4/6 kinase blockade [ Haematologica, 2022, 10.3324/haematol.2021.279848] PubMed: 35021603
Establishment and Characterization of NCC-PMP1-C1: A Novel Patient-Derived Cell Line of Metastatic Pseudomyxoma Peritonei [ J Pers Med, 2022, 12(2)258] PubMed: 35207746
Establishment and characterization of immortalized sweat gland myoepithelial cells [ Sci Rep, 2022, 12(1):7] PubMed: 34997030

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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

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