Decernotinib

Research use only, not for human use.

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.

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.

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VX-509 | VRT-831509

Angiogenesis

JAK

JAK1|JAK2|JAK3|Tyk2

Inflammation/Immunology

Rheumatoid Arthritis

944842-54-0

392.3783

C18H19F3N6O

>98% (HPLC)

10 mM in DMSO

CC[C@](NC1=NC(C2=CNC3=NC=CC=C32)=NC=C1)(C)C(NCC(F)(F)F)=O.

Butanamide, 2-methyl-2-[[2-(1H-pyrrolo[2,3-b]pyridin-3-yl)-4-pyrimidinyl]amino]-N-(2,2,2-trifluoroethyl)-, (2R)-

(-20℃)

With Ice Pack

≥ 2 years