GLPG0634-analogue
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MedKoo CAT#: 407355

CAS#: 1206101-20-3

Description: GLPG0634-analogue is an analogue of Filgotinib or GLPG0634, is a potent and selective JAK1 inhibitor.


Chemical Structure

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GLPG0634-analogue
CAS# 1206101-20-3

Theoretical Analysis

MedKoo Cat#: 407355
Name: GLPG0634-analogue
CAS#: 1206101-20-3
Chemical Formula: C23H18N6O2
Exact Mass: 410.1491
Molecular Weight: 410.437
Elemental Analysis: C, 67.31; H, 4.42; N, 20.48; O, 7.80

Price and Availability

Size Price Availability Quantity
100.0mg USD 850.0 2 Weeks
200.0mg USD 1450.0 2 Weeks
500.0mg USD 2150.0 2 Weeks
1.0g USD 3250.0 2 Weeks
2.0g USD 4850.0 2 Weeks
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Related CAS #: 1206161-97-8   1206101-20-3  

Synonym: Filgotinib-analogue, GLPG0634-analogue; GLPG0634 analogue; GLPG-0634 analogue; GLPG 0634 analogue.

IUPAC/Chemical Name: N-[5-[4-[(6-Cyano-3-pyridinyl)methoxy]phenyl][1,2,4]triazolo[1,5-a]pyridin-2-yl]-cyclopropanecarboxamide

InChi Key: QZXABVVSCDZCLR-UHFFFAOYSA-N

InChi Code: InChI=1S/C23H18N6O2/c24-12-18-9-4-15(13-25-18)14-31-19-10-7-16(8-11-19)20-2-1-3-21-26-23(28-29(20)21)27-22(30)17-5-6-17/h1-4,7-11,13,17H,5-6,14H2,(H,27,28,30)

SMILES Code: O=C(C1CC1)NC2=NN3C(C4=CC=C(OCC5=CC=C(C#N)N=C5)C=C4)=CC=CC3=N2

Appearance: 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

Shelf Life: >2 years if stored properly

Drug Formulation: This drug may be formulated in DMSO

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 410.437 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.

Recalculate based on batch purity %
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.



Additional Information

Related CAS#
CAS#1206161-97-8 (Filgotinib, GLPG0634)
CAS#1206101-20-3 (Filgotinib-analogue, GLPG0634-analogue)