Filgotinib
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MedKoo CAT#: 206136

CAS#: 1206161-97-8

Description: Filgotinib, also known as GLPG0634, is a potent and selective JAK1 inhibitor under investigation for the treatment of rheumatoid arthritis (RA) and Crohn's disease. It is considered a promising agent as it inhibits JAK1 selectively. Filgotinib displayed a selectivity of 30-fold for JAK1- over JAK2-dependent signaling. GLPG0634 dose-dependently inhibited Th1 and Th2 differentiation and to a lesser extent the differentiation of Th17 cells in vitro.


Chemical Structure

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Filgotinib
CAS# 1206161-97-8

Theoretical Analysis

MedKoo Cat#: 206136
Name: Filgotinib
CAS#: 1206161-97-8
Chemical Formula: C21H23N5O3S
Exact Mass: 425.15216
Molecular Weight: 425.5
Elemental Analysis: C, 59.28; H, 5.45; N, 16.46; O, 11.28; S, 7.54

Size Price Shipping out time Quantity
25mg USD 150 Same day
50mg USD 250 Same day
100mg USD 450 Same day
200mg USD 750 Same day
500mg USD 1250 Same day
1g USD 2150 Same day
2g USD 3850 2 weeks
5g USD 6950 2 weeks
Inquire bulk and customized quantity

Pricing updated 2021-03-03. Prices are subject to change without notice.

Filgotinib (GLPG0634), purity > 98%, is in stock. The same day shipping out after order is received.

Related CAS #: 1206161-97-8   1206101-20-3  

Synonym: GLPG0634; GLPG 0634; GLPG-0634. Filgotinib; PubChemSID 163643231

IUPAC/Chemical Name: N-(5-(4-((1,1-dioxidothiomorpholino)methyl)phenyl)-[1,2,4]triazolo[1,5-a]pyridin-2-yl)cyclopropanecarboxamide.

InChi Key: RIJLVEAXPNLDTC-UHFFFAOYSA-N

InChi Code: InChI=1S/C21H23N5O3S/c27-20(17-8-9-17)23-21-22-19-3-1-2-18(26(19)24-21)16-6-4-15(5-7-16)14-25-10-12-30(28,29)13-11-25/h1-7,17H,8-14H2,(H,23,24,27)

SMILES Code: O=C(C1CC1)NC2=NN3C(C4=CC=C(CN5CCS(CC5)(=O)=O)C=C4)=CC=CC3=N2.

Appearance:
White to off-white-solid powder

Purity:
>98% (or refer to the Certificate of Analysis)

Shipping Condition:
Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.

Storage Condition:
Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).

Solubility:
Soluble in DMSO, not in water

Shelf Life:
>2 years if stored properly

Drug Formulation:
GLPG0634 was formulated in polyethyleneglycol 200/0.9% NaCl (60/40; v/v) for i.v. administration and in 0.5% (v/v) methylcellulose for oral administration for all in vivo studies

Stock Solution Storage:
0 - 4 C for short term (days to weeks), or -20 C for long term (months).

HS Tariff Code:
2934.99.9001

Preparing Stock Solutions

The following data is based on the product molecular weight 425.5 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Select a batch to recalculate based on the batch molecular weight:
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 1.15 mL 5.76 mL 11.51 mL
5 mM 0.23 mL 1.15 mL 2.3 mL
10 mM 0.12 mL 0.58 mL 1.15 mL
50 mM 0.02 mL 0.12 mL 0.23 mL

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1: Nakayamada S, Kubo S, Iwata S, Tanaka Y. Recent Progress in JAK Inhibitors for the Treatment of Rheumatoid Arthritis. BioDrugs. 2016 Aug 31. Review. Erratum in: BioDrugs. 2016 Oct 3;:. PubMed PMID: 27577235.

2: Roskoski R Jr. Janus kinase (JAK) inhibitors in the treatment of inflammatory and neoplastic diseases. Pharmacol Res. 2016 Sep;111:784-803. doi: 10.1016/j.phrs.2016.07.038. Epub 2016 Jul 26. Review. PubMed PMID: 27473820.

3: Liu CY, Li Q, Zhou XD. [Inhibition of suppressor of cytokine signaling 1 on lipopolysaccharide-induced mucin5AC hypersecretion and the mechanism in human bronchial epithelial cells]. Zhonghua Yi Xue Za Zhi. 2016 Mar 29;96(12):966-70. doi: 10.3760/cma.j.issn.0376-2491.2016.12.012. Chinese. PubMed PMID: 27045723.

4: Nielsen OH, Seidelin JB, Ainsworth M, Coskun M. Will novel oral formulations change the management of inflammatory bowel disease? Expert Opin Investig Drugs. 2016 Jun;25(6):709-18. doi: 10.1517/13543784.2016.1165204. Epub 2016 Mar 28. PubMed PMID: 26967267.

5: Namour F, Desrivot J, Van der Aa A, Harrison P, Tasset C, van't Klooster G. Clinical Confirmation that the Selective JAK1 Inhibitor Filgotinib (GLPG0634) has a Low Liability for Drug-drug Interactions. Drug Metab Lett. 2016;10(1):38-48. PubMed PMID: 26693854.

6: Namour F. Author's Reply to Srinivas: "Pharmacokinetics and Pharmacokinetic/Pharmacodynamic Modeling of Filgotinib (GLPG0634), a Selective JAK1 Inhibitor, in Support of Phase IIB Dose Selection". Clin Pharmacokinet. 2015 Dec;54(12):1297-8. doi: 10.1007/s40262-015-0336-5. PubMed PMID: 26482170; PubMed Central PMCID: PMC4661215.

7: Srinivas NR. Comment on: "Pharmacokinetics and Pharmacokinetic/Pharmacodynamic Modelling of Filgotinib (GLPG0634), a Selective JAK1 Inhibitor, in Support of Phase IIB Dose Selection". Clin Pharmacokinet. 2015 Dec;54(12):1293-5. doi: 10.1007/s40262-015-0335-6. PubMed PMID: 26482169.

8: Namour F, Diderichsen PM, Cox E, Vayssière B, Van der Aa A, Tasset C, Van't Klooster G. Pharmacokinetics and Pharmacokinetic/Pharmacodynamic Modeling of Filgotinib (GLPG0634), a Selective JAK1 Inhibitor, in Support of Phase IIB Dose Selection. Clin Pharmacokinet. 2015 Aug;54(8):859-74. doi: 10.1007/s40262-015-0240-z. PubMed PMID: 25681059; PubMed Central PMCID: PMC4513223.

9: Menet CJ, Fletcher SR, Van Lommen G, Geney R, Blanc J, Smits K, Jouannigot N, Deprez P, van der Aar EM, Clement-Lacroix P, Lepescheux L, Galien R, Vayssiere B, Nelles L, Christophe T, Brys R, Uhring M, Ciesielski F, Van Rompaey L. Triazolopyridines as selective JAK1 inhibitors: from hit identification to GLPG0634. J Med Chem. 2014 Nov 26;57(22):9323-42. doi: 10.1021/jm501262q. Epub 2014 Nov 17. PubMed PMID: 25369270.

10: Norman P. Selective JAK inhibitors in development for rheumatoid arthritis. Expert Opin Investig Drugs. 2014 Aug;23(8):1067-77. doi: 10.1517/13543784.2014.918604. Epub 2014 May 12. Review. PubMed PMID: 24818516.



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