Decernotinib (VX-509) - 10mM in DMSO, high purity , CAS No.944842-54-0

Item Number

D427037

• Synonyms: Butanamide, 2-methyl-2-((2-(1H-pyrrolo(2,3-b)pyridin-3-yl)-4-pyrimidinyl)amino)-N-(2,2,2-trifluoroethyl)-, (2R)- | F18308 | NCGC00402345-03 | VX 509 | Decernotinib(VX-509) | Decernotinib (VX-509,adelatinib) | Decernotinib [USAN:INN] | MZK2GP0RHK | (2R)-2-
• Specifications & Purity: Moligand™, 10mM in DMSO
• Biochemical and Physiological Mechanisms: Decernotinib (VX-509) is a potent and selective JAK3 inhibitor with K_i of 2.5 nM, >4-fold selectivity over JAK1, JAK2, and TYK2, respectively. Phase 2/3.
• Storage Temp: Store at -80°C
• Shipped In: Ice chest + Ice pads
• Grade: Moligand™

Product Description

Information

Decernotinib (VX-509) is a potent and selectiveJAK3inhibitor withKiof 2.5 nM, >4-fold selectivity over JAK1, JAK2, and TYK2, respectively. Phase 2/3.

Targets

JAK3 ; JAK1 ; JAK1 ; JAK2 ; TYK2 2.5 nM(Ki); 11 nM; 11 nM(Ki); 13 nM(Ki); 13 nM(Ki)

In vitro

In 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 vivo

In 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