Cat. No.: HY-18300A

Filgotinib maleate

(Synonyms: GLPG0634 maleate)

28 Cited Publications

Customer Review

Based on 28 publication(s) in Google Scholar

Filgotinib maleate (GLPG0634 maleate) is a selective, orally available JAK1 inhibitor with anti-inflammatory and antiviral activities. Filgotinib maleate can effectively inhibit the activities of JAK1, JAK2, JAK3 and TYK2 with IC₅₀ values of 10 nM, 28 nM, 810 nM and 116 nM, respectively. Filgotinib maleate also inhibits HIV-1 driven gene transcription and reduces proliferation of HIV-1 infected cells. Filgotinib maleate can be used in the study of rheumatoid arthritis and inflammatory bowel disease.

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

Purity: 99.88%
CAS No.: 1802998-75-9
Formula: C₂₅H₂₇N₅O₇S
Molecular Weight:541.58

Storage:

4°C, sealed storage, away from moisture

* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

Filgotinib maleate Chemical Structure

CAS No.: 1802998-75-9

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Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biological Activity
- Description
- IC₅₀ & Target
- In Vitro
- In Vivo
Chemical Information
Publications (28)
Solvent & Solubility
- In Vitro
Purity & Documentation
References
Help & FAQs
Classifications
Bioz

Biological Activity

Description

IC₅₀ & Target^[1]

JAK1

10 nM (IC₅₀)

JAK2

28 nM (IC₅₀)

JAK3

810 nM (IC₅₀)

Tyk2

116 nM (IC₅₀)

All JAK Isoforms :

All HIV Isoforms :

In Vitro

Filgotinib maleate (0.1, 1 and 10 μM) inhibits the differentiation of Th2 cells and Th1 cells in a dose-dependent manner^[1].

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

In Vivo

Filgotinib maleate (0.1, 0.3, 1, 3, 10 and 30 mg/kg, i.g.; once daily for 15 days) produces dose-dependent bone damage protection and prevents the development of inflammation in a rat model of collagen-induced arthritis^[1].

Pharmacokinetic analysis of GLPG0634 in mice^[1]

Route	Dose (mg/kg)	C₀ or C₀ (ng/mL)	T_max (h)	T_1/2 (h)	Cl (L•h/kg)	V_ss (L/kg)	F (%)
i.v.	1	637	/	2.5	2.9	6	/
p.o.	5	920	0.5	1.7	/	/	100

Pharmacokinetic analysis of GLPG0634 in rats^[1]

Route	Dose (mg/kg)	C₀ or C₀ (ng/mL)	T_max (h)	T_1/2 (h)	Cl (L•h/kg)	V_ss (L/kg)	F (%)
i.v.	1	1407	/	1.6	1.4	1.8	/
p.o.	5	310	2.2	3.9	/	/	45

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

Animal Model:

therapeutic rat CIA model^[1]
Dosage:

0.1, 0.3, 1, 3, 10 and 30 mg/kg
Administration:

i.g. 1 time per day for 15 days
Result:

Reduced inflammatory cell infiltration while protecting articular cartilage and bone at a dose of 1 mg/kg.
Reduced serum levels of inflammatory cytokines and chemokines including IL-6, IP-10, XCL1, and MCP-1.

Chemical Information

CAS No. 1802998-75-9
Appearance Solid
Molecular Weight 541.58
Formula C₂₅H₂₇N₅O₇S
Color White to off-white
SMILES

OC(/C=C\C(O)=O)=O.O=C(C1CC1)NC2=NN3C(C4=CC=C(C=C4)CN5CCS(=O)(CC5)=O)=CC=CC3=N2
Synonyms

GLPG0634 maleate
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

4°C, sealed storage, away from moisture

* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

Publications (28)

All RT-PCRWB

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Journal Impact Factor

Nature

Coronaviruses exploit a host cysteine-aspartic protease for replication. [Abstract]

2022 Sep;609(7928):785-792. PMID: 35922005
Science

The target landscape of clinical kinase drugs. [Abstract]

2017 Dec 1;358(6367):eaan4368. PMID: 29191878
Nat Cancer

Ectopic JAK-STAT activation enables the transition to a stem-like and multilineage state conferring AR-targeted therapy resistance. [Abstract]

2022 Sep;3(9):1071-1087. PMID: 36065066
Nat Commun

Human iPSC-based Modeling of Pulmonary Fibrosis Reveals p300/CBP Inhibition Suppresses Alveolar Transitional Cell State. [Abstract]

2026 Feb 12;17(1):1214. PMID: 41680175
Nat Commun

Co-targeting JAK1/STAT6/GAS6/TAM signaling improves chemotherapy efficacy in Ewing sarcoma. [Abstract]

2024 Jun 21;15(1):5292. PMID: 38906855
MedComm (2020)

Loss of Adenosine Deaminase Acting on RNA 1 Induces Panoptosis and Immune Response in Ulcerative Colitis Gut Mucosa. [Abstract]

2025 Jun 6;6(6):e70212. PMID: 40487746
NPJ Precis Oncol

Filgotinib inhibits METTL3-mediated m6A of EIF3A by targeting ERG-TBP to suppress PDAC progression JAK-STAT3-independently. [Abstract]

2026 Apr 1;10(1):193. PMID: 41922492
Oncogene

microRNA-23a, -27a and -24 synergistically regulate JAK1/Stat3 cascade and serve as novel therapeutic targets in human acute erythroid leukemia. [Abstract]

2016 Nov 17;35(46):6001-6014. PMID: 27086927
Apoptosis

USP9X regulates copper-induced CASP9/CASP3/GSDME-dependent pyroptosis by deubiquitinating JAK1. [Abstract]

2026 Jun 18;31(7):177. PMID: 42315669
Leukemia

Stem cell persistence in CML is mediated by extrinsically activated JAK1-STAT3 signaling. [Abstract]

2019 Aug;33(8):1964-1977. PMID: 30842608
J Med Chem

Synthetic Strategy and Evaluation of the Benzyloxy Benzylamide Derivatives as Thymic Stromal Lymphopoietin Modulators for the Treatment of Atopic Dermatitis. [Abstract]

2025 Dec 30. PMID: 41467342
Virulence

Immunosuppressants exert antiviral effects against influenza A(H1N1)pdm09 virus via inhibition on nucleic acid synthesis, mRNA splicing and protein stability. [Abstract]

2024 Dec;15(1):2301242. PMID: 38170681

Filgotinib maleate purchased from MedChemExpress. Usage Cited in: Virulence. 2024 Dec;15(1):2301242. [Abstract]

Filgotinib (0.1, 1, 10 μM) significantly reduced IAV RNA level. Viral RNA was quantified by qRT-PCR after 36 h Filgotinib treatment and compared to control group.

Filgotinib maleate purchased from MedChemExpress. Usage Cited in: Virulence. 2024 Dec;15(1):2301242. [Abstract]

Filgotinib (0.1, 1, 10 μM) inhibited IAV HA and NP accumulation. Samples were subjected to western blot and HA and NP were detected.
Mol Syst Biol

Illuminating phenotypic drug responses of sarcoma cells to kinase inhibitors by phosphoproteomics. [Abstract]

2024 Jan;20(1):28-55. PMID: 38177929
Drug Des Devel Ther

Drug Interaction Potential of Berberine Hydrochloride When Co-Administered with Tofacitinib and Filgotinib in Rats. [Abstract]

2025 Jun 10:19:5043-5057. PMID: 40524804
Eur J Pharmacol

Trim65 attenuates isoproterenol-induced cardiac hypertrophy by promoting autophagy and ameliorating mitochondrial dysfunction via the Jak1/Stat1 signaling pathway. [Abstract]

2023 Jun 15:949:175735. PMID: 37080331
Molecules

Development of an LC-MS/MS Method for Quantification of Sapitinib in Human Liver Microsomes: In Silico and In Vitro Metabolic Stability Evaluation. [Abstract]

2023 Mar 2;28(5):2322. PMID: 36903565
Molecules

Assessment of In Silico and In Vitro Selpercatinib Metabolic Stability in Human Liver Microsomes Using a Validated LC-MS/MS Method. [Abstract]

2023 Mar 14;28(6):2618. PMID: 36985590
Hum Gene Ther

Knockout-Induced Pluripotent Stem Cells for Disease and Therapy Modeling of IL-10-Associated Primary Immunodeficiencies. [Abstract]

2021 Jan;32(1-2):77-95. PMID: 33023317
J Virol

Porcine reproductive and respiratory syndrome virus N protein-mediated viral replication enhancement via interaction with host caspase-6. [Abstract]

2026 May 19;100(5):e0016326. PMID: 41979901
J Immunol

Complex Regulation Pattern of IRF3 Activation Revealed by a Novel Dimerization Reporter System. [Abstract]

2016 May 15;196(10):4322-30. PMID: 27045107
PLoS Genet

Systems biology of tissue-specific response to Anaplasma phagocytophilum reveals differentiated apoptosis in the tick vector Ixodes scapularis. [Abstract]

2015 Mar 27;11(3):e1005120. PMID: 25815810
J Steroid Biochem Mol Biol

Interleukin-2 receptor γ blocks the development of Leydig cells from stem/progenitor cells in male rats via JAK1-STAT3 pathway and GSDMD-mediated pyroptosis. [Abstract]

2026 May:259:106953. PMID: 41662993
J Chromatogr B Analyt Technol Biomed Life Sci

Development and validation of an HPLC-MS/MS method for the determination of filgotinib, a selective Janus kinase 1 inhibitor: Application to a metabolic stability study. [Abstract]

2020 Oct 1:1154:122195. PMID: 32943176
SSRN

2025 Sep 3.
Patent

US20250161243A1.
bioRxiv

2025 February 21.
bioRxiv

2024 September 24.
bioRxiv

02 Nov 2021.

Solvent & Solubility

In Vitro:

DMSO : 35 mg/mL (64.63 mM; ultrasonic and warming and heat to 60°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

1.8464 mL

9.2322 mL

18.4645 mL

5 mM

0.3693 mL

1.8464 mL

3.6929 mL

10 mM

0.1846 mL

0.9232 mL

1.8464 mL

Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.

Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Molarity Calculator

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

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Purity & Documentation

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (282 KB)
SDS (418 KB)
- English - EN (418 KB)
- Français - FR (418 KB)
- Deutsch - DE (418 KB)
- Norwegian - NO (418 KB)
- Español - ES (418 KB)
- Swedish - SV (418 KB)
- Italian - IT (418 KB)
- Korean - KR (418 KB)
- Portuguese - PT (418 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

References

[1]. Van Rompaey L, et, al. Preclinical characterization of GLPG0634, a selective inhibitor of JAK1, for the treatment of inflammatory diseases. J Immunol. 2013 Oct 1;191(7):3568-77. [Content Brief]

[2]. Labetoulle R, et al. Filgotinib for the treatment of Crohn's disease. Expert Opin Investig Drugs. 2018 Mar;27(3):295-300. [Content Brief]

[3]. Yeh, et al. "Filgotinib suppresses HIV-1–driven gene transcription by inhibiting HIV-1 splicing and T cell activation." The Journal of Clinical Investigation 130.9 (2020): 4969-4984. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	1.8464 mL	9.2322 mL	18.4645 mL	46.1612 mL
	5 mM	0.3693 mL	1.8464 mL	3.6929 mL	9.2322 mL
	10 mM	0.1846 mL	0.9232 mL	1.8464 mL	4.6161 mL
	15 mM	0.1231 mL	0.6155 mL	1.2310 mL	3.0774 mL
	20 mM	0.0923 mL	0.4616 mL	0.9232 mL	2.3081 mL
	25 mM	0.0739 mL	0.3693 mL	0.7386 mL	1.8464 mL
	30 mM	0.0615 mL	0.3077 mL	0.6155 mL	1.5387 mL
	40 mM	0.0462 mL	0.2308 mL	0.4616 mL	1.1540 mL
	50 mM	0.0369 mL	0.1846 mL	0.3693 mL	0.9232 mL
	60 mM	0.0308 mL	0.1539 mL	0.3077 mL	0.7694 mL

Keywords

Filgotinib maleate

28 Cited Publications

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Filgotinib maleate

Bioactive Compound Library Max

Bioactive Compound Library

Anti-Infection Compound Library

Epigenetics Compound Library

Immunology/Inflammation Compound Library

JAK/STAT Compound Library

Kinase Inhibitor Library

Protein Tyrosine Kinase Compound Library

Stem Cell Signaling Compound Library

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Publications Citing Use of MedChemExpress (MCE) Filgotinib maleate

All JAK Isoforms

All HIV Isoforms

Biological Activity

Chemical Information

Publications (28)

Solvent & Solubility

Purity & Documentation

References

Help & FAQs

Complete Stock Solution Preparation Table

Filgotinib maleate Related Classifications

HY-18300A Related Classifications