Molecular Weight(MW): 425.50
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.
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Confocal microscopy showing BAFF in ductal epithelial structures within SG organoids from patients with sicca (Sc) or primary Sjögren's syndrome (SS). Nuclei were stained with DAPI (blue). Original magnification × 100.
Arthritis Rheumatol, 2018, 70(12):2057-2066. Filgotinib (GLPG0634) purchased from Selleck.
Treatment of IL-6 (10 ng/ml) with or without S3I-201 (a STAT3 antagonist, 5 μM) or filgotinib (a JAK1 inhibitor, 10 nM). Mean ± SEM, n = 6. *, **,*** indicate significant difference between two groups when compared to the control at P < 0.05, 0.01, 0.001, respectively.
Mol Cell Endocrinol, 2018, 472:26-39. Filgotinib (GLPG0634) purchased from Selleck.
Purity & Quality Control
Choose Selective JAK Inhibitors
|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.|
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 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.  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. |
|In vitro||DMSO||85 mg/mL (199.76 mM)|
|In vivo||Add solvents to the product individually and in order(Data is from Selleck tests instead of citations):
4% DMSO+30% PEG 300+ddH2O
For best results, use promptly after mixing.
* 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.
Calculate the mass, volume or concentration required for a solution. The Selleck molarity calculator is based on the following equation:
Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)
*When preparing stock solutions, please always use the batch-specific molecular weight of the product found on the via label and MSDS / COA (available on product pages).
Calculate the dilution required to prepare a stock solution. The Selleck dilution calculator is based on the following equation:
Concentration (start) x Volume (start) = Concentration (final) x Volume (final)
This equation is commonly abbreviated as: C1V1 = C2V2 ( Input Output )
* When preparing stock solutions always use the batch-specific molecular weight of the product found on the vial label and MSDS / COA (available online).
Molecular Weight Calculator
Enter the chemical formula of a compound to calculate its molar mass and elemental composition:
Tip: Chemical formula is case sensitive. C10H16N2O2 c10h16n2o2
Instructions to calculate molar mass (molecular weight) of a chemical compound:
To calculate molar mass of a chemical compound, please enter its chemical formula and click 'Calculate'.
Definitions of molecular mass, molecular weight, molar mass and molar weight:
Molecular mass (molecular weight) is the mass of one molecule of a substance and is expressed in the unified atomic mass units (u). (1 u is equal to 1/12 the mass of one atom of carbon-12)
Molar mass (molar weight) is the mass of one mole of a substance and is expressed in g/mol.
Clinical Trial Information
|NCT Number||Recruitment||Conditions||Sponsor/Collaborators||Start Date||Phases|
|NCT03417778||Completed||Rheumatoid Arthritis|Ulcerative Colitis|Crohn''s Disease||Gilead Sciences|Galapagos NV||April 3 2018||Phase 1|
|NCT03285711||Recruiting||Lupus Membranous Nephropathy||Gilead Sciences||October 6 2017||Phase 2|
|NCT03320876||Active not recruiting||Psoriatic Arthritis||Galapagos NV||July 26 2017||Phase 2|
|NCT03207815||Recruiting||Noninfectious Uveitis||Gilead Sciences||July 26 2017||Phase 2|
|NCT03201445||Recruiting||Ulcerative Colitis||Gilead Sciences|Galapagos NV||July 11 2017||Phase 2|
|NCT03134222||Recruiting||Cutaneous Lupus Erythematosus||Gilead Sciences|Galapagos NV||May 24 2017||Phase 2|
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.
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Frequently Asked Questions
Could you recommemd a vehicle for oral gavage for S7605?
It can be dissolved in 5% Tween 80+0.5% CMC Na at 30 mg/ml as a suspension for oral gavage.