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Filgotinib | JAK1 inhibitor

CAS:
1206161-97-8
Catalog Number:
10-5145
Activity:
JAK1 inhibitor
Chemical Names:
N-[5-[4-[(1,1-dioxido-4-thiomorpholinyl)methyl]phenyl][1,2,4]triazolo[1,5-ɑ]pyridin-2-yl]-cyclopropanecarboxamide
GLPG0634; GS-6034
Molecular Weight:
425.50
Molecular Formula:
C21H23N5O3S
Solubility:
Soluble in DMSO (15 mg/ml with warming)
Physical Properties:
Off-white solid
Purity:
98% TLC
NMR (Conforms)
Storage Temperature:
-20°C
Stability:
Stable for 2 years from date of purchase as supplied. Solutions in DMSO may be stored at -20°C for up to 1 month.
Shipping Code:
RT

Filgotinib (1206161-97-8) is a potent and selective JAK1 inhibitor (IC50s=10, 28, 810 and 116 nM for JAK1, JAK2, JAK3 and TYK2 respectively).2  Displays potent anti-inflammatory activity in various models.1,2  Effective as a monotherapy in patients with active rheumatoid arthritis.3 Reverses oncostatin M-mediated inhibition of rat stem Leydig cell differentiation.4

References:

  1. Menet et al. (2014), Triazolopyridines as selective JAK1 inhibitors: from hit identification to GLPG0634; Med. Chem., 57 9323
  2. Rompaey et al. (2013), Preclinical characterization of GLPG0634, a selective inhibitor of JAK1, for the treatment of inflammatory diseases; Immunol., 191 3568
  3. Kavanaugh et al. (2017), Filgotinib (GLPG0634/GS-6034), an oral selective JAK1 inhibitor, is effective as monotherapy in patients with active rheumatoid arthritis: results from a randomized dose-finding study (DARWIN 2); Rheum. Dis., 76 1009
  4. Wang et al.  (2019), Oncostatin M inhibits differentiation of rat stem Leydig cells in vivo and in vitro; J. Cell. Mol. Med., 23 426
Filgotinib | JAK1 inhibitor is also available in the Cellular Metabolism Library.
CAS:
1206161-97-8
Catalog Number:
10-5145
Activity:
JAK1 inhibitor
Chemical Names:
N-[5-[4-[(1,1-dioxido-4-thiomorpholinyl)methyl]phenyl][1,2,4]triazolo[1,5-ɑ]pyridin-2-yl]-cyclopropanecarboxamide
GLPG0634; GS-6034
Molecular Weight:
425.50
Molecular Formula:
C21H23N5O3S
Solubility:
Soluble in DMSO (15 mg/ml with warming)
Physical Properties:
Off-white solid
Purity:
98% TLC
NMR (Conforms)
Storage Temperature:
-20°C
Stability:
Stable for 2 years from date of purchase as supplied. Solutions in DMSO may be stored at -20°C for up to 1 month.
Shipping Code:
RT

Safety Data Sheet:

N/A

Product Data Sheet:

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