Decernotinib
Decernotinib (VX-509, VRT-831509) is a potent, selective, orally available JAK3 inhibitor with Ki of 2.5 nM and cellular IC50 of 50-170 nM, demonstrates limited inhibition of JAK1/JAK2/TYK2 in cell-based assays (25-100 fold) ; also inhibits JAK1, JAK2 and TYK2 (Ki=11, 13 and 11 nM) in biochemical assay and shows >400-fold selectivity over a broad kinases; inhibits IL-2–induced STAT-5 phosphorylation in IL-2–dependent T-cell line with IC50 of 99 nM, potently suppresses T-cell proliferation with IC50 of 170 nM; modulates proinflammatory response in models of immune-mediated diseases, such as collagen-induced arthritis and delayed-type hypersensitivity.Rheumatoid Arthritis Phase 2 Discontinued.
Product Specifications
CAS Number
944842-54-0
Product Name Alternative
VX-509 | VRT-831509
Purity
>98% (HPLC)
Solubility
10 mM in DMSO
Smiles
CC[C@] (NC1=NC (C2=CNC3=NC=CC=C32) =NC=C1) (C) C (NCC (F) (F) F) =O.
Molecular Formula
C18H19F3N6O
Molecular Weight
392.3783
Storage Conditions
Storage temperature: -20°C. Stability: ≥ 2 years
Notes
For research use only.
Other Product Names
Butanamide, 2-methyl-2-[[2- (1H-pyrrolo[2,3-b]pyridin-3-yl) -4-pyrimidinyl]amino]-N- (2,2,2-trifluoroethyl) -, (2R) -
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