Decernotinib (VX-509) (C007B-137872)

InformationDecernotinib (VX-509) is a potent and selectiveJAK3inhibitor withKiof 2.5 nM, >4-fold selectivity over JAK1, JAK2, and TYK2, respectively. Phase 2/3.TargetsJAK3 ; JAK1 ; JAK1 ; JAK2 ; TYK2 2.5 nM(Ki); 11 nM; 11 nM(Ki); 13 nM(Ki); 13 nM(Ki)In vitroIn HT-2 cells, Decernotinib inhibits IL-2–stimulated HT-2 STAT-5 phosphorylation, human T-cell blast proliferation, and CD40L/IL-4–induced B-cell proliferation.In vivoIn a rat model of collagen-induced arthritis, VX-509 (50 mg/kg, p.o.) results in dose-dependent reduction in ankle swelling and paw weight and improved paw histopathology scores. In a mouse model of oxazolone-induced delayed-type hypersensitivity, VX-509 (50 mg/kg, p.o.) significantly suppresses ear edema. In a rat HvG model, VX-509 (50 mg/kg, p.o.) results in dose-dependent inhibition of popletial lymph node (PLN) hyperplasia.Cell Research(from reference)Cell lines：Human B cells Concentrations：~1 μM Incubation Time：6 d.

Specifications and Purity: 10mM in DMSO

Molecular Formula: C18H19F3N6O

Molecular Weight: 392.38

PubChem CID: 59422203

Isomeric SMILES: CC[C@](C)(C(=O)NCC(F)(F)F)NC1=NC(=NC=C1)C2=CNC3=C2C=CC=N3