Art. -Nr.: HY-18300

Filgotinib

(Synonyms: GLPG0634)

28 Cited Publications

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Based on 28 publication(s) in Google Scholar

Filgotinib (GLPG0634) is a selective, orally available JAK1 inhibitor with anti-inflammatory and antiviral activities. Filgotinib 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 also inhibits HIV-1 driven gene transcription and reduces proliferation of HIV-1 infected cells. Filgotinib can be used in the study of rheumatoid arthritis and inflammatory bowel disease.

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Reinheit: 99.77%
CAS. Nr.: 1206161-97-8
Formel: C₂₁H₂₃N₅O₃S
Molecular Weight:425.50

Speicherung:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month

Filgotinib Chemical Structure

CAS. Nr.: 1206161-97-8

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Top Publications Citing

Use of MCE Products

Fluorescent Dye

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

Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
- Clinical Trial
Chemical Information
Publications (28)
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

IC₅₀ & Target^[1]

JAK1

10 nM (IC₅₀)

JAK2

28 nM (IC₅₀)

Tyk2

116 nM (IC₅₀)

JAK3

810 nM (IC₅₀)

Alle JAK Isoform-spezifische Produkte anzeigen :

Alle HIV Isoform-spezifische Produkte anzeigen :

Cellular Effect

Cell Line	Type	Value	Description	References
BaF3	IC₅₀	4546 nM Compound: GLPG0634	Antiproliferative activity against mouse BaF3 cells assessed as IL-3-induced inhibition of cell growth incubated for 40 hrs Antiproliferative activity against mouse BaF3 cells assessed as IL-3-induced inhibition of cell growth incubated for 40 hrs	[PMID: 24006460]
BaF3	IC₅₀	4546 nM Compound: 65, GLPG0634	Inhibition of JAK2 in IL3-induced human BaF3 cells assessed as cell proliferation Inhibition of JAK2 in IL3-induced human BaF3 cells assessed as cell proliferation	[PMID: 25369270]
BaF3	IC₅₀	1.43 μM Compound: 5	Inhibition of JAK1 (unknown origin) expressed in mouse BAF3 cells assessed as antiproliferative activity by cell-based assay Inhibition of JAK1 (unknown origin) expressed in mouse BAF3 cells assessed as antiproliferative activity by cell-based assay	[PMID: 32527540]
BaF3	IC₅₀	13.26 μM Compound: 5	Inhibition of JAK3 (unknown origin) expressed in mouse BAF3 cells assessed as antiproliferative activity by cell-based assay Inhibition of JAK3 (unknown origin) expressed in mouse BAF3 cells assessed as antiproliferative activity by cell-based assay	[PMID: 32527540]
BaF3	IC₅₀	4.45 μM Compound: 5	Inhibition of JAK2 (unknown origin) expressed in mouse BAF3 cells assessed as antiproliferative activity by cell-based assay Inhibition of JAK2 (unknown origin) expressed in mouse BAF3 cells assessed as antiproliferative activity by cell-based assay	[PMID: 32527540]
CWR22R	IC₅₀	>10000 nM Compound: 65, GLPG0634	Inhibition of JAK2 in PRL-induced human 22Rv1 cells assessed as pSTAT5 Inhibition of JAK2 in PRL-induced human 22Rv1 cells assessed as pSTAT5	[PMID: 25369270]
HeLa	IC₅₀	1045 nM Compound: 65, GLPG0634	Inhibition of JAK1/JAK2 in OSM-induced human HeLa cells assessed as STAT1 reporter Inhibition of JAK1/JAK2 in OSM-induced human HeLa cells assessed as STAT1 reporter	[PMID: 25369270]
T-cell	IC₅₀	1.127 nM Compound: GLPG0634	Inhibition of JAK1/TYK2 in human whole blood assessed as reduction in IFN-alpha-induced STAT1 phosphorylation in CD4+ T cells preincubated with compound for 30 mins followed by IFN-alpha addition and measured after 20 mins by flow cytometry analysis Inhibition of JAK1/TYK2 in human whole blood assessed as reduction in IFN-alpha-induced STAT1 phosphorylation in CD4+ T cells preincubated with compound for 30 mins followed by IFN-alpha addition and measured after 20 mins by flow cytometry analysis	[PMID: 24006460]
T-cell	IC₅₀	17453 nM Compound: GLPG0634	Inhibition of JAK2 in human whole blood assessed as reduction in GM-CSF-induced STAT5 phosphorylation in CD3-positive T cell preincubated with compound for 30 mins followed by GM-CSF addition and measured after 20 mins by flow cytometry analysis Inhibition of JAK2 in human whole blood assessed as reduction in GM-CSF-induced STAT5 phosphorylation in CD3-positive T cell preincubated with compound for 30 mins followed by GM-CSF addition and measured after 20 mins by flow cytometry analysis	[PMID: 24006460]
T-cell	IC₅₀	1789 nM Compound: GLPG0634	Inhibition of JAK1/JAK3 in human whole blood assessed as reduction in IL-2-induced STAT5 phosphorylation in CD4+ T cells preincubated with compound for 30 mins followed by IL-2 addition and measured after 20 mins by flow cytometry analysis Inhibition of JAK1/JAK3 in human whole blood assessed as reduction in IL-2-induced STAT5 phosphorylation in CD4+ T cells preincubated with compound for 30 mins followed by IL-2 addition and measured after 20 mins by flow cytometry analysis	[PMID: 24006460]
T-cell	IC₅₀	629 nM Compound: GLPG0634	Inhibition of JAK1 in human whole blood assessed as reduction in IL6-induced STAT1 phosphorylation in CD4+ T cells preincubated with compound for 30 mins followed by IL-6 addition and measured after 20 mins by flow cytometry analysis Inhibition of JAK1 in human whole blood assessed as reduction in IL6-induced STAT1 phosphorylation in CD4+ T cells preincubated with compound for 30 mins followed by IL-6 addition and measured after 20 mins by flow cytometry analysis	[PMID: 24006460]
TF-1	IC₅₀	3524 nM Compound: 65, GLPG0634	Inhibition of JAK2 in IL3-induced human TF1 cells assessed as pSTAT5 Inhibition of JAK2 in IL3-induced human TF1 cells assessed as pSTAT5	[PMID: 25369270]
THP-1	IC₅₀	154 nM Compound: 65, GLPG0634	Inhibition of JAK1/JAK3 in IL4-induced human THP1 cells assessed as pSTAT6 Inhibition of JAK1/JAK3 in IL4-induced human THP1 cells assessed as pSTAT6	[PMID: 25369270]
THP-1	IC₅₀	3364 nM Compound: 65, GLPG0634	Inhibition of JAK1/JAK2 in IFNgamma-induced human THP1 cells assessed as pSTAT1 Inhibition of JAK1/JAK2 in IFNgamma-induced human THP1 cells assessed as pSTAT1	[PMID: 25369270]
U2OS	IC₅₀	436 nM Compound: 65, GLPG0634	Inhibition of JAK1/TYK2 in IFN-alphaB2-induced human U2OS cells assessed as pSTAT1 Inhibition of JAK1/TYK2 in IFN-alphaB2-induced human U2OS cells assessed as pSTAT1	[PMID: 25369270]

In Vitro

Filgotinib (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 (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.

Clinical Trial

NCT Number	Sponsor	Condition	Start Date	Phase A549
NCT01329991	Plexxikon\|		2011-05	PHASE1

Chemical Information

CAS. Nr. 1206161-97-8
Appearance Solid
Molecular Weight 425.50
Formel C₂₁H₂₃N₅O₃S
Color Off-white to gray
SMILES

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

GLPG0634
Versand

Room temperature in continental US; may vary elsewhere.

Speicherung

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

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 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 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.

Lösungsmittel & Löslichkeit

In Vitro:

DMSO : 25 mg/mL (58.75 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

H₂O : < 0.1 mg/mL (insoluble)

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

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. 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. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Molaritätsrechner

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

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

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