A JAK1 inhibitor (IC50 = 10 nM); selective for JAK1 over JAK3 (IC50 = 810 nM) but also inhibits JAK2 and Tyk2 (IC50s = 28 and 116 nM

Filgotinib – 10 mg

Brand:
Cayman
CAS:
1206161-97-8
Storage:
-20
UN-No:
Non-Hazardous - /

Filgotinib is a JAK1 inhibitor (IC50 = 10 nM).{30750} 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.  

 

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Description

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

Formal name: N-[5-[4-[(1,1-dioxido-4-thiomorpholinyl)methyl]phenyl][1,2,4]triazolo[1,5-ɑ]pyridin-2-yl]-cyclopropanecarboxamide

Synonyms:  GLPG0634

Molecular weight: 425.5

CAS: 1206161-97-8

Purity: ≥98%

Formulation: A crystalline solid

Product Type|Biochemicals|Kinase Inhibitors|JAK Family||Product Type|Biochemicals|Small Molecule Inhibitors|Kinases||Research Area|Cell Biology|Cell Signaling|JAK Signaling||Research Area|Epigenetics, Transcription, & Translation|Transcription Factors||Research Area|Immunology & Inflammation|Adaptive Immunity||Research Area|Immunology & Inflammation|Autoimmunity|Rheumatoid Arthritis||Research Area|Immunology & Inflammation|Innate Immunity

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