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Filgotinib (GLPG0634) JAK inhibitor

Name: Filgotinib (GLPG0634)
Brand: Selleck Chemicals
SKU: S7605
Availability: InStock
Rating: 5 (49 reviews)

Cat.No.S7605

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, and is in Phase 2.

Chemical Structure

Molecular Weight: 425.50

Jump to Mechanism of Action Cell Culture & Working Concentration Solubility Chemical Information, Storage & Stability Specificity

Quality Control

Batch: Purity: 99.76%

99.76

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Cell Culture, Treatment & Working Concentration

Cell Lines	Assay Type	Incubation Time	Activity Description	PMID
human CD34+ cells	Function assay	45 mins	Inhibition of JAK2 homodimer in human CD34+ cells spiked into human whole blood assessed as inhibition of EPO-induced STAT-5 phosphorylation preincubated for 45 mins followed by EPO addition measured after 15 mins by FACS analysis	24417533
NK92	Function assay		Inhibition of JAK1/JAK3 in IL2-induced human NK92 cells assessed as pSTAT5, =0.148μM.	25369270
THP1	Function assay		Inhibition of JAK1/JAK3 in IL4-induced human THP1 cells assessed as pSTAT6, =0.154μM.	25369270
U2OS	Function assay		Inhibition of JAK1/TYK2 in IFN-alphaB2-induced human U2OS cells assessed as pSTAT1, =0.436μM.	25369270
HeLa	Function assay		Inhibition of JAK1/JAK2 in OSM-induced human HeLa cells assessed as STAT1 reporter, =1.045μM.	25369270
THP1	Function assay		Inhibition of JAK1/JAK2 in IFNgamma-induced human THP1 cells assessed as pSTAT1, =3.364μM.	25369270
TF1	Function assay		Inhibition of JAK2 in IL3-induced human TF1 cells assessed as pSTAT5, =3.524μM.	25369270
BaF3	Function assay		Inhibition of JAK2 in IL3-induced human BaF3 cells assessed as cell proliferation, =4.546μM.	25369270
SJ-GBM2	qHTS assay		qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SJ-GBM2 cells	29435139
A673	qHTS assay		qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for A673 cells	29435139
SK-N-MC	qHTS assay		qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-MC cells	29435139
BT-37	qHTS assay		qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-37 cells	29435139
NB-EBc1	qHTS assay		qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB-EBc1 cells	29435139
Saos-2	qHTS assay		qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Saos-2 cells	29435139
NB1643	qHTS assay		qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB1643 cells	29435139
BT-12	qHTS assay		qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-12 cells	29435139
RD	qHTS assay		qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for RD cells	29435139
MG 63 (6-TG R)	qHTS assay		qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for MG 63 (6-TG R) cells	29435139
Click to View More Cell Line Experimental Data

Chemical Information, Storage & Stability

Molecular Weight	425.50	Formula	C₂₁H₂₃N₅O₃S	Storage (From the date of receipt)	3 years-20°Cpowder
CAS No.	1206161-97-8	Download SDF		Storage of Stock Solutions	1 year-80°Cin solvent 1 month-20°Cin solvent
Synonyms	N/A			Smiles	C1CC1C(=O)NC2=NN3C(=N2)C=CC=C3C4=CC=C(C=C4)CN5CCS(=O)(=O)CC5

Solubility

In vitro
Batch:

DMSO : 21 mg/mL (49.35 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Water : Insoluble

Ethanol : Insoluble

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
=	×	×

Dilution Calculator Molecular Weight Calculator

In vivo Batch:
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	4%DMSO 1 30%PEG300 2 66%ddH2O Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	3.000mg/ml (7.05mM)	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.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	1.400mg/ml (3.29mM)	Taking the 1 mL working solution as an example, add 50 μL of 28 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

Dosage: mg/kg Average weight of animals: g Dosing volume per animal:μL Number of animals:

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO + % + % Tween 80 + % ddH₂O

%DMSO+ %

Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH₂O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Mechanism of Action

Targets/IC₅₀/Ki	JAK1 ^[1] (Cell-free assay) 10 nM JAK2 ^[1] (Cell-free assay) 28 nM TYK2 ^[1] (Cell-free assay) 116 nM JAK3 ^[1] (Cell-free assay) 810 nM
In vitro	Filgotinib (GLPG0634) inhibits IL-2- and IL-4-induced JAK1/JAK3/γc signaling and IFN-αB2-induced JAK1/TYK2 type II receptor signaling with IC50 values ranging from 150 to 760 nM in cell lines. It shows higher selectivity for JAK/STAT signaling involving JAK1 than JAK2 kinase in a cellular context. Besides, this compound also inhibits the differentiation of Th1, Th2, and Th17 cells. ^[1]
In vivo	Following oral administration, the absolute bioavailability of filgotinib (GLPG0634) is moderate in rats (45%) and high in mice (∼100%). This compound (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] In DSS-treated mice, it 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]
References	[1] https://pubmed.ncbi.nlm.nih.gov/24006460/ [2] https://www.ecco-ibd.eu/index.php/publications/congress-abstract-s/abstracts-2014/item/p072-glpg0634-the-first-selective-jak1-inhibitor-shows-strong-activity-in-the-mouse-dss-colitis-model.html

Applications

Methods	Biomarkers	Images	PMID
Western blot	p-STAT3 / STAT3		28191885

Clinical Trial Information

(data from https://clinicaltrials.gov, updated on 2024-05-22)

NCT Number	Recruitment	Conditions	Sponsor/Collaborators	Start Date	Phases
NCT06222034	Recruiting	Juvenile Idiopathic Arthritis	Galapagos NV	April 2024	Phase 1
NCT06043739	Completed	Bioavailability	Galapagos NV	September 22 2023	Phase 1
NCT05697159	Recruiting	Rheumatoid Arthritis\|Sickness Behavior\|Inflammatory Disease\|Autoimmune\|Pain Chronic	NHS Greater Glasgow and Clyde\|Galapagos NV	August 22 2023	--
NCT05653791	Active not recruiting	Ulcerative Colitis	Academisch Medisch Centrum - Universiteit van Amsterdam (AMC-UvA)\|Galapagos NV	October 1 2022	--
NCT03417778	Completed	Rheumatoid Arthritis	Gilead Sciences\|Galapagos NV	April 3 2018	Phase 1

Tech Support

Handling Instructions

Tel: +1-832-582-8158 Ext:3

If you have any other enquiries, please leave a message.

Frequently Asked Questions

Question 1:
Could you recommend a vehicle for oral gavage for it?

Answer:
It can be dissolved in 5% Tween 80+0.5% CMC Na at 30 mg/ml as a suspension for oral gavage.

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