[CAS NO. 944842-54-0] Decernotinib (VX-509)

Name: Decernotinib (VX-509)
Brand: Arctom Scientific
SKU: SLK-S7541

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PRODUCTS SPECIFICATIONS [944842-54-0]

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Catalog

SLK-S7541

Brand

Selleck

CAS

944842-54-0

DESCRIPTION [944842-54-0]

Overview

MDL	MFCD27987896
Molecular Weight	392.38
Molecular Formula	C18H19F3N6O
SMILES	N([C@@](C(NCC(F)(F)F)=O)(CC)C)C1=NC(C=2C=3C(NC2)=NC=CC3)=NC=C1

For research use only.

Storage

3 years,-20°C,powder
1 years,-80°C,in solvent

Shipping

Room temperature shipping(Stability testing shows this product can be shipped without any cooling measures.)

Preparing Stock Solutions

Concentration Volume Mass	1 mg	5 mg	10 mg
1 mM	2.5485 mL	12.7427 mL	25.4855 mL
5 mM	0.5097 mL	2.5485 mL	5.0971 mL
10 mM	0.2549 mL	1.2743 mL	2.5485 mL
50 mM	0.0510 mL	0.2549 mL	0.5097 mL

Description

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

Targets

JAK3 ^[1]	JAK1 ^[1]	JAK1 ^[1]	JAK2 ^[1]	TYK2 ^[1]
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.

References

[1] Mahajan S, et al. J Pharmacol Exp Ther. 2015, 353(2), 405-414.
[2] Farmer LJ, et al. J Med Chem. 2015, 58(18), 7195-7216.

Synonyms

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

(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

Decernotinib

V 509

(2R)-2-Methyl-2-[[2-(1H-pyrrolo[2,3-b]pyridin-3-yl)pyrimidin-4-yl]amino]-N-(2,2,2-trifluoroethyl)butanamide