An internal standard for the quantification of filgotinib
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Unlabeled Version(s)
17669Filgotinib
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Filgotinib-d4

Item No. 28875

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
N-[5-[4-[(1,1-dioxido-4-thiomorpholinyl)methyl]phenyl][1,2,4]triazolo[1,5-a]pyridin-2-yl]-cyclopropane-2,2,3,3-d4-carboxamide
CAS Number
2041095-50-3
Synonyms
  • GLPG0634-d4
Molecular Formula
C21H19D4N5O3S
Formula Weight
429.5
Purity
≥99% deuterated forms (d1-d4)
Formulation (Request formulation change)
A solid
Solubility(Learn about Variance in Solubility)
Acetonitrile:Methanol (1:1): solubleDMSO: soluble
SMILES
O=S1(CCN(CC2=CC=C(C3=CC=CC4=NC(NC(C5C([2H])([2H])C5([2H])[2H])=O)=NN43)C=C2)CC1)=O
InChi Code
InChI=1S/C21H23N5O3S/c27-20(17-8-9-17)23-21-22-19-3-1-2-18(26(19)24-21)16-6-4-15(5-7-16)14-25-10-12-30(28,29)13-11-25/h1-7,17H,8-14H2,(H,23,24,27)/i8D2,9D2
InChi Key
RIJLVEAXPNLDTC-LZMSFWOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    1 mg

    $358

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    Product Description

    Filgotinib-d4 is intended for use as an internal standard for the quantification of filgotinib (Item No. 17669) by GC- or LC-MS. Filgotinib is a JAK1 inhibitor (IC50 = 10 nM).1 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.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Van Rompaey, L., Galien, R., van der Aar, E.M., et al. Preclinical characterization of GLPG0634, a selective inhibitor of JAK1, for the treatment of inflammatory diseases. J. Immunol. 191(7), 3568-3577 (2013).