MedKoo Cat#: 407355 | Name: GLPG0634-analogue
Featured

Description:

WARNING: This product is for research use only, not for human or veterinary use.

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

Chemical Structure

GLPG0634-analogue
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: 410.44

Elemental Analysis: C, 67.31; H, 4.42; N, 20.48; O, 7.80

Price and Availability

Size Price Availability Quantity
100mg USD 850.00 4 Weeks
200mg USD 1,450.00 4 Weeks
500mg USD 2,150.00 4 Weeks
1g USD 3,250.00 4 Weeks
Bulk Inquiry
Buy Now
Add to Cart
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
More Info
Related CAS# CAS#1206161-97-8 (Filgotinib, GLPG0634) CAS#1206101-20-3 (Filgotinib-analogue, GLPG0634-analogue)
Product Data
Biological target:
GLPG0634 analog (Compound 176) is a broad spectrum JAK inhibitor with IC50 values of <100 nM against JAK1, JAK2 and JAK3.
In vitro activity:
TBD
In vivo activity:
TBD
Solvent mg/mL mM
Solubility
DMSO 53.0 129.13
Note: There can be variations in solubility for the same chemical from different vendors or different batches from the same vendor. The following factors can affect the solubility of the same chemical: solvent used for crystallization, residual solvent content, polymorphism, salt versus free form, degree of hydration, solvent temperature. Please use the solubility data as a reference only. Warming and sonication will facilitate dissolving. Still have questions? Please contact our Technical Support scientists.

Preparing Stock Solutions

The following data is based on the product molecular weight 410.44 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
Formulation protocol:
TBD
In vitro protocol:
TBD
In vivo protocol:
TBD
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.