2. Epigenetics Stem Cell/Wnt Protein Tyrosine Kinase/RTK JAK/STAT Signaling
  3. JAK
  4. Filgotinib

Filgotinib  (Synonyms: GLPG0634)

Cat. No.: HY-18300 Purity: 99.68%
COA Handling Instructions

Filgotinib (GLPG0634) is a selective and orally active 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

Size Price Stock Quantity
Free Sample (0.1 - 0.5 mg)   Apply Now  
Solution
10 mM * 1 mL in DMSO USD 101 In-stock
Solid + Solvent
10 mM * 1 mL
ready for reconstitution
 USD 101 In-stock
Solid
5 mg USD 92 In-stock
10 mg USD 145 In-stock
25 mg USD 238 In-stock
50 mg USD 370 In-stock
100 mg USD 634 In-stock
200 mg   Get quote  
500 mg   Get quote  

* Please select Quantity before adding items.

This product is a controlled substance and not for sale in your territory.

Customer Review

Based on 14 publication(s) in Google Scholar

Other Forms of Filgotinib:

Filgotinib Related Antibodies

Top Publications Citing Use of Products

View All JAK Isoform Specific Products:

View All Isoforms
JAK1 JAK2 JAK3 Tyk2 JAK

  • Biological Activity

  • Protocol

  • Purity & Documentation

  • References

  • Customer Review

Description

Filgotinib (GLPG0634) is a selective and orally active JAK1 inhibitor with IC50 of 10 nM, 28 nM, 810 nM, and 116 nM for JAK1, JAK2, JAK3, and TYK2, respectively.

IC50 & Target[1]

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].

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

Filgotinib Related Antibodies
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].

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

425.50

Appearance

Solid

Formula

C21H23N5O3S
CAS No.
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 : 25 mg/mL (58.75 mM; Need ultrasonic)

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.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.5 mg/mL (5.88 mM); Clear solution

  • 2.

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.5 mg/mL (5.88 mM); Clear solution

  • 3.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 2.5 mg/mL (5.88 mM); Clear solution

  • 4.

    Add each solvent one by one:  5% DMSO    40% PEG300    5% Tween-80    50% saline

    Solubility: ≥ 2.5 mg/mL (5.88 mM); Clear solution

  • 5.

    Add each solvent one by one:  5% DMSO    95% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.5 mg/mL (5.88 mM); Clear solution

*All of the co-solvents are available by MCE.
Purity & Documentation

Purity: 99.68%

COA (252 KB) LCMS (93 KB)

Handling Instructions (2659 KB)
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
  • No file chosen (Maximum size is: 1024 Kb)
  • If you have published this work, please enter the PubMed ID.
  • Your name will appear on the site.

Filgotinib Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

  • Molarity Calculator

  • Dilution Calculator

The molarity calculator equation

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass   Concentration   Volume   Molecular Weight *
= × ×

The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
× = ×
C1   V1   C2   V2

Keywords:

Filgotinib1206161-97-8GLPG0634GLPG 0634GLPG-0634JAKJanus kinaseInhibitorinhibitorinhibit

Your Recently Viewed Products:

Inquiry Online

Your information is safe with us. * Required Fields.

Product Name

  

Salutation

Applicant Name *

 

Email Address *

Phone Number *

 

Organization Name *

Department *

 

Requested quantity *

Country or Region *

      

Remarks

Bulk Inquiry

Inquiry Information

Product Name:
Filgotinib
Cat. No.:
HY-18300
Quantity:
MCE Japan Authorized Agent:

Customer Review

Thank You for Your Feedback!

Request for HNMR Report

Please fill out this form to request the QC report. We will send it to your Email address shortly.

Your information is safe with us. * Required Fields.

Product Name

  

Lot #

Applicant Name *

 

Email Address *

Phone Number

 

Department *

Organization Name *

 

Country or Region *

Remarks

Request for HNMR Report

We have received your request and will respond to you as soon as possible.