GLPG-0634 (FILGOTINIB)

Background Information:

GLPG0634 (Filgotinib)* is the first orally-available, selective
inhibitor of JAK1. In vitro, it selectively inhibits JAK1 and JAK2 with
IC50 values of 10 nM and 28 nM, respectively, selective over JAK3 and
TYK2 (IC50 Values of 810 nM and 116 nM, respectively), and a panel of
150 other kinases. However, when tested in vivo it selectively inhibits
JAK1, displaying a 30-fold potency over JAK2. It is currently in
clinical evaluation for immune-inflammatory associated diseases.

Reference:

1. L. Van Rompaey, et al., Preclinical characterization of GLPG0634, a
selective inhibitor of JAK1, for the treatment of inflammatory
diseases, J Immunol. 2013 Oct 1, 191(7):3568-77.* The structure has been
disclosed by authoritative sources. A wrong structure of this product,
with CAS No: 1206101-20-3, Empirical Formula: C23H18N6O2, Mol. Wt:
410.43, is being offered in marketplace. Buyer beware!!

APIM050156: GLPG-0634 (FILGOTINIB)

CAS No.: 1206161-97-8.
Molecular Formula: C₂₁H₂₃N₅O₃S?0.2H₂O.
Molecular Weight: 429.1.
Purity: >99% (HPLC at 214 and 254 nm).
QC: HPLC-MS, ¹HNMR, and Quantitative Elemental Analysis.
Solubility: Soluble in DMSO.
Storage: Store at 0°C (short term), -20°C (long term), desiccated.