Filgotinib

ChemicalBook > CAS DataBase List > Filgotinib

Description In vitro In vivo

Product Name: Filgotinib
CAS No.: 1206161-97-8
Chemical Name: Filgotinib
Synonyms: GLPG0634;SYN1158;GLPG634;CS-1083;GPLG0634;Feigotini;filgotinib;GLPG0634 >=95%;GLPG0634 (analog);GLPG0634;GLPG 0634
CBNumber: CB52621138
Molecular Formula: C21H23N5O3S
Formula Weight: 425.5
MOL File: 1206161-97-8.mol

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Filgotinib Property

Melting point:: 229 - 231°C
Density: 1.51±0.1 g/cm3(Predicted)
storage temp.: -20°C
solubility: Soluble in DMSO (15 mg/ml with warming)
form: solid
pka: 8.04±0.20(Predicted)
color: Off-white
Stability:: Stable for 2 years from date of purchase as supplied. Solutions in DMSO may be stored at -20°C for up to 1 month.

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Safety

HS Code: 2921309990

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Hazard and Precautionary Statements (GHS)

Symbol(GHS)

Signal word

Warning

Hazard statements

H315Causes skin irritation

H319Causes serious eye irritation

H335May cause respiratory irritation

Precautionary statements

P264Wash hands thoroughly after handling.

P264Wash skin thouroughly after handling.

P280Wear protective gloves/protective clothing/eye protection/face protection.

P302+P352IF ON SKIN: wash with plenty of soap and water.

P305+P351+P338IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continuerinsing.

P321Specific treatment (see … on this label).

P332+P313IF SKIN irritation occurs: Get medical advice/attention.

P362Take off contaminated clothing and wash before reuse.

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N-Bromosuccinimide Price

Cayman Chemical

Product number: 17669
Product name: Filgotinib
Purity: ≥98%
Packaging: 5mg
Price: $56
Updated: 2024/03/01

Cayman Chemical

Product number: 17669
Product name: Filgotinib
Purity: ≥98%
Packaging: 1mg
Price: $25
Updated: 2021/12/16

Cayman Chemical

Product number: 17669
Product name: Filgotinib
Purity: ≥98%
Packaging: 10mg
Price: $99
Updated: 2024/03/01

Cayman Chemical

Product number: 17669
Product name: Filgotinib
Purity: ≥98%
Packaging: 25mg
Price: $166
Updated: 2024/03/01

TRC

Product number: G411100
Product name: GLPG-0634(Filgotinib)
Packaging: 25mg
Price: $200
Updated: 2021/12/16

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Filgotinib Chemical Properties,Usage,Production

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.

In vitro

In cell lines, GLPG0634 inhibits IL-2- and IL-4-induced JAK1/JAK3/γc signaling and IFN-αB2-induced JAK1/TYK2 type II receptor signaling with IC50 ranged from 150 to 760 nM. GLPG0634 shows higher selectivity for JAK/STAT signaling involving JAK1 than JAK2 kinase in a cellular context. Besides, GLPG0634 also inhibits the differentiation of Th1, Th2, and Th17 cells.

In vivo

Following oral administration, the absolute bioavailability is moderate in rats (45%) and high in mice (～100%). Filgotinib (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. Filgotinib (GLPG0634) in DSS-treated mice 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.

Description

Filgotinib is a JAK1 inhibitor (IC₅₀ = 10 nM). It is selective for JAK1 over JAK3 (IC₅₀ = 810 nM) but also inhibits JAK2 and tyrosine kinase 2 (Tyk2; IC₅₀s = 28 and 116 nM, respectively), as well as Abl, FLT1, -3, and -4, FMS, Mer, and TBK1 activity by greater than 35% in a panel of 177 tyrosine kinases at 1 μM. Filgotinib inhibits IL-6-induced phosphorylation of STAT1 in CD4⁺ T cells with an IC₅₀ value of 629 nM in isolated human whole blood. It reduces hind paw macrophage and T cell infiltration and bone erosion in a rat model of collagen-induced arthritis when administered at doses ranging from 0.1 to 30 mg/kg per day for 15 days.

Uses

GLPG-0634 (Filgotinib) is a potent, selective JAK1 inhibitor. Used as an anti-inflammatory agent, it reduces levels of inflammatory cytokines in the bones and tissue of mammals.

Mechanism of action

Filgotinib acts on the JAK-STAT pathway by selectively inhibiting JAK1 phosphorylation and preventing STAT activation, which ultimately results in reduced proinflammatory cytokine signaling.

Side effects

feeling sick (nausea)
upper respiratory tract infection
urinary tract infection.
dizziness.

Synthesis

The synthesis of Filgotinib is as follows:
With cyclopropanyl chloride in an amidated reaction in a system consisting of N-methylmorpholine and 1,4-dioxane,The amidation reaction time was 4 h,The amidation reaction temperature was 50 ° C,The molar ratio of the intermediate (III), cyclopropanyl chloride, N-methylmorpholine and 1,4-dioxane was 1: 2.8: 2.5:TLC plate to determine the reaction is completed, cooled to room temperature,Adding methylene chloride and water, separating the organic phase with water,Then washed with brine, dried over magnesium sulfate,Evaporated to dryness and the residue was purified over a silica gel column [elution solvent: ethyl acetate / n-hexane (3: 7 v / v)To obtain a solid yellowish solid,That is, Filgotinib, yield 91.2%.

References

Menet et al. (2014), Triazolopyridines as selective JAK1 inhibitors: from hit identification to GLPG0634; Med. Chem., 57 9323 Rompaey et al. (2013), Preclinical characterization of GLPG0634, a selective inhibitor of JAK1, for the treatment of inflammatory diseases; Immunol., 191 3568 Kavanaugh et al. (2017), Filgotinib (GLPG0634/GS-6034), an oral selective JAK1 inhibitor, is effective as monotherapy in patients with active rheumatoid arthritis: results from a randomized dose-finding study (DARWIN 2); Rheum. Dis., 76 1009 Wang et al. ?(2019), Oncostatin M inhibits differentiation of rat stem Leydig cells in vivo and in vitro; J. Cell. Mol. Med., 23 426

Filgotinib Preparation Products And Raw materials

Raw materials

Preparation Products

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View Lastest Price from Filgotinib manufacturers

shandong perfect biotechnology co.ltd

Product: GLPG0634 1206161-97-8
Price: US $0.00/g
Min. Order: 1g
Purity: 98% HPLC
Supply Ability: 1kg
Release date: 2023-08-01

Hebei Mingeng Biotechnology Co., Ltd

Product: GLPG0634 ,Filgotinib 1206161-97-8
Price: US $150.00/ASSAYS
Min. Order: 10g
Purity: more than 99.6%
Supply Ability: 500kg/month
Release date: 2021-12-03

Zhejiang J&C Biological Technology Co.,Limited

Product: GPLG0634 1206161-97-8
Price: US $0.00/gram
Min. Order: 1gram
Purity: 99%
Supply Ability: 10kg
Release date: 2022-02-17

1206161-97-8, FilgotinibRelated Search:

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GPLG0634

GLPG0634

SYN1158

CyclopropanecarboxaMide, N-[5-[4-[(1,1-dioxido-4-thioMorpholinyl)Methyl]phenyl][1,2,4]triazolo[1,5-a]pyridin-2-yl]-

GLPG0634 (analog)

N-[5-[4-[(1,1-Dioxido-4-thiomorpholinyl)methyl]phenyl][1,2,4]triazolo[1,5-a]pyridin-2-yl]cyclopropanecarboxamide

N-(5-(4-((1,1-Dioxidothiomorpholino)methyl)phenyl)-[1,2,4]triazolo[1,5-a]pyridin-2-yl)cyclopropanecarboxamide

Filgotinib (GLPG0634)

N-[5-[4-[(1,1-Dioxido-4-thiomorpholinyl)methyl]phenyl][1,2,4]triazolo[1,5-a]pyridin-2-yl]cyclopropanecarboxamide Filgotinib (GLPG0634)

GLPG0634(filgotinib)

GLPG634

N-(5-(4-((1,1-Dioxidothiomorpholino)methyl)phenyl)-[1,2,4]triazolo[1,5-a]pyridin-2-yl)cyclopro

GLPG0634 >=95%

GLPG0634;GLPG 0634;FILGOTINIB

GPLG0634，filgotinib

GLPG0634;GLPG 0634

CS-1083

N-(5-{4-[(1,1-Dioxidothiomorpholin-4-yl)methyl]phenyl}[1,2,4]triazolo[1,5-a]pyridin-2-yl)cyclopropanecarboxamide (2Z)-but-2-enedioate

GPLG0634 USP/EP/BP

filgotinib

Feigotini

cyclopropanecarboxylic acid {5-[ 4-(1,1-dioxo-thiomorpholin-4-ylmethyl)-phenyl]-[1,2,4]triazolo[1,5-a]pyridin-2-yl}-amide

GLPG 0634,GLPG-0634,inhibit,Janus kinase,JAK,Filgotinib,Inhibitor

N-[5-[4-[(1,1-dioxo-1,4-thiazinan-4-yl)methyl]phenyl]-[1,2,4]triazolo[1,5-a]pyridin-2-yl]cyclopropanecarboxamide

1206161-97-8

Inhibitors

API

1206161-97-8