1. Epigenetics
    Stem Cell/Wnt
    JAK/STAT Signaling
  2. JAK
  3. Filgotinib

Filgotinib (Synonyms: GLPG0634)

Cat. No.: HY-18300 Purity: 99.64%
Handling Instructions

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.

For research use only. We do not sell to patients.

Filgotinib Chemical Structure

Filgotinib Chemical Structure

CAS No. : 1206161-97-8

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25 mg USD 216 In-stock
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50 mg USD 336 In-stock
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100 mg USD 576 In-stock
Estimated Time of Arrival: December 31
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Customer Review

Based on 6 publication(s) in Google Scholar

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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.

IC50 & Target

JAK1

10 nM (IC50)

JAK2

28 nM (IC50)

Tyk2

116 nM (IC50)

JAK3

810 nM (IC50)

In Vitro

Filgotinib (GLPG0634) dose-dependently inhibits the differentiation of Th2 cells mediated by IL-4, a cytokine that signals through JAK1 and JAK3. Filgotinib also inhibits Th1 differentiation with similar potencies of 1 μM or lower[1]. Filgotinib (GLPG0634) does not inhibit JAK2 homodimer-mediated signaling induced by EPO or PRL (IC50 > 10 μM)[2].

In Vivo

Filgotinib (GLPG0634; 3, 10, 30 mg/kg, p.o.) dose-dependently prevents disease progression in the therapeutic rat CIA model. Filgotinib (50 mg/kg, o.p.) protects bone and cartilage from degradation, effectively reduces infiltration of T cells (CD3+ cells) and macrophages (F4/80+ cells) in the paw, and decreases the serum levels of all cytokines and chemokines measured, including IL-6, IP-10, XCL1, and MCP-1[1]. Filgotinib (GLPG0634; 0.1 and 0.3 mg/kg) shows efficacy in the rat CIA model[2].

Clinical Trial
Molecular Weight

425.50

Formula

C₂₁H₂₃N₅O₃S

CAS No.

1206161-97-8

SMILES

O=C(C1CC1)NC2=NN3C(C4=CC=C(CN5CCS(CC5)(=O)=O)C=C4)=CC=CC3=N2

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 6.8 mg/mL (15.98 mM; Need ultrasonic and warming)

H2O : < 0.1 mg/mL (insoluble)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.3502 mL 11.7509 mL 23.5018 mL
5 mM 0.4700 mL 2.3502 mL 4.7004 mL
10 mM 0.2350 mL 1.1751 mL 2.3502 mL
*Please refer to the solubility information to select the appropriate solvent.
References
Animal Administration
[1]

Filgotinib is orally dosed as a single esophageal gavage at 5 mg/kg (dosing volume of 5 mL/kg) and i.v. dosed as a bolus via the caudal vein at 1 mg/kg (dosing volume of 5 mL/kg). In the rat study, each group consists of three rats and blood samples are collected via the jugular vein. In the mouse study, each group consists of 21 mice (n=3/time point) and blood samples are collected by intracardiac puncture under isoflurane anesthesia. Lithium heparin is used as anticoagulant and blood is taken at 0.05, 0.25, 0.5, 1, 3, 5, and 8 h (i.v. route) and 0.25, 0.5, 1, 3, 5, 8, and 24 h (by mouth).

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

References

Purity: 99.64%

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Keywords:

FilgotinibGLPG0634GLPG 0634GLPG-0634JAKJanus kinaseInhibitorinhibitorinhibit

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