DC Chemicals · Product datasheet

Decernotinib (VX-509,adelatinib) — Datasheet

CAT. NO. DC8171

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ParameterValue
Chemical NameDecernotinib
CAS No.944842-54-0
SynonymsVX-509;decernotinib;(2R)-2-methyl-2-[[2-(1H-pyrrolo[2,3-b]pyridin-3-yl)pyrimidin-4-yl]amino]-N-(2,2,2-trifluoroethyl)butanamide;VRT-831509;(2R)-2-Methyl-2-[[2-(1H-pyrrolo[2,3-b]pyridin-3-yl)-4-pyrimidinyl]amino]-N-(2,2,2-trifluoroethyl)butanamide;VRT 831509;VX 509;Adelatinib;MZK2GP0RHK;AK170453;(2r)-2-Methyl-2-[[2-(1h-Pyrrolo[2,3-B]pyridin-3-Yl)pyrimidin-4-Yl]amino]-N-[2,2,2-Tris(Fluoranyl)ethyl]butanamide;(R)-2-((2-(1H-Pyrrolo[2,3-b]pyridin-3-yl)pyrimidin-4-yl)amino)-2-methyl-N-(2,2,2-trifluoroethyl)butanamide;VX509;Decernotinib [USAN:INN];Decernotinib (USAN/INN)
FormulaC18H19F3N6O
M.Wt392.3783
SMILESFC(C([H])([H])N([H])C([C@@](C([H])([H])[H])(C([H])([H])C([H])([H])[H])N([H])C1C([H])=C([H])N=C(C2=C([H])N([H])C3=C2C([H])=C([H])C([H])=N3)N=1)=O)(F)F
Purity>98%
Storage2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO

Biological Activity

Decernotinib is a potent, orally active JAK3 inhibitor, with Kis of 2.5, 11, 13 and 11 nM for JAK3, JAK1, JAK2, and TYK2, respectively.

In Vitro

Decernotinib (VX-509) is a potent JAK3 inhibitor, with Kis of 2.5, 11, 13 and 11 nM for JAK3, JAK1, JAK2, and TYK2, respectively. Decernotinib potently blocks T-cell proliferation with a mean IC50 of 170 ± 101 nM, and inhibits IL-2-stimulated T-cell proliferation (IC50, 140 and 400 nM). VX-509 is also cytotoxic to B-cell in response to CD40L and IL-4 (IC50, 50 nM)[1].

In Vivo

Decernotinib (VX-509, 10, 25, or 50 mg/kg, p.o.) significantly and dose-dependently inhibits the increases in ankle diameter and paw weight occuring in response to collagen injections in rats. Decernotinib potently alleviates cartilage damage and bone resorption in rats. Decernotinib (10, 25, or 50 mg/kg, p.o., b.i.d.) suppresses ear edema in a mouse model of delayed-type hypersensitivity[1].

References & source

DC Chemicals original product information

Published experimental findings depend on the model and assay conditions. They do not guarantee equivalent performance in every application. For laboratory research use only.

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