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959754-85-9

959754-85-9 Structure

959754-85-9 Structure
IdentificationBack Directory
[Name]

4-(8-((4-(4-(tert-butyl)piperazin-1-yl)phenyl)aMino)-[1,2,4]triazolo[1,5-a]pyrazin-5-yl)furan-2-carboxaMide
[CAS]

959754-85-9
[Synonyms]

4-(8-((4-(4-(tert-Butyl)piperazin-1-yl)phenyl)amino)-[1,2,4]triazolo[1,5-a]pyrazin-5-yl)furan-
4-(8-((4-(4-(tert-Butyl)piperazin-1-yl)phenyl)amino)-[1,2,4]triazolo[1,5-a]pyrazin-5-yl)furan-2-c
4-[8-[4-(4-tert-butylpiperazin-1-yl)anilino]-[1,2,4]triazolo[1,5-a]pyrazin-5-yl]furan-2-carboxamide
4-(8-((4-(4-(tert-butyl)piperazin-1-yl)phenyl)aMino)-[1,2,4]triazolo[1,5-a]pyrazin-5-yl)furan-2-carboxaMide
2-Furancarboxamide, 4-[8-[[4-[4-(1,1-dimethylethyl)-1-piperazinyl]phenyl]amino][1,2,4]triazolo[1,5-a]pyrazin-5-yl]-
[Molecular Formula]

C24H28N8O2
[MDL Number]

MFCD22419398
[MOL File]

959754-85-9.mol
[Molecular Weight]

460.53
Chemical PropertiesBack Directory
[density ]

1.39±0.1 g/cm3(Predicted)
[storage temp. ]

2-8°C
[form ]

Solid
[pka]

15.21±0.50(Predicted)
[color ]

Off-white to yellow
Hazard InformationBack Directory
[Uses]

GLPG0259 is a ATP-competitive inhibitor of MAPK-activated protein kinase 5 (MK5) with oral activity. GLPG0259 reduces inflammation and bone destruction in a mouse model of collagen-induced arthritis. GLPG0259 also inhibited the metastasis of prostate cancer (PCa) cells[1][2].
[in vivo]

GLPG0259 (2 mg/kg, 10 mg/kg; i.p.; twice weekly for 7 weeks) impairs tumor cells lung metastasis in SCID beige mice bearing prostate cancer (PCa) cell lines P3 cells (i.v.)[1].

[References]

[1] Westhovens R, et al. Oral administration of GLPG0259, an inhibitor of MAPKAPK5, a new target for the treatment of rheumatoid arthritis: a phase II, randomised, double-blind, placebo-controlled, multicentre trial. Ann Rheum Dis. 2013 May;72(5):741-4. DOI:10.1136/annrheumdis-2012-202221
[2] Khalil MI, et al. The TLK1-MK5 Axis Regulates Motility, Invasion, and Metastasis of Prostate Cancer Cells. Cancers (Basel). 2022 Nov 22;14(23):5728. DOI:10.3390/cancers14235728
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