Decernotinib

SKU: orb1305235

Description

Decernotinib (VX-509) is a potent and selective JAK3 inhibitor with a Ki of 2.5 nM. It demonstrates cellular activity (IC50 50-170 nM) and has been investigated in preclinical models of autoimmune diseases, including rheumatoid arthritis, for its immunomodulatory effects.

Research Area

Cardiovascular Research, Epigenetics & Chromatin, Signal Transduction, Stem Cell & Developmental Biology

Images & Validation

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Key Properties

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CAS Number	944842-54-0
MW	392.38
Purity	99.64%
Formula	C₁₈H₁₉F₃N₆O
SMILES	CC[C@@](C)(Nc1ccnc(n1)-c1c[nH]c2ncccc12)C(=O)NCC(F)(F)F
Target	JAK,Tyrosine Kinases
Solubility	Ethanol:16 mg/mL (40.78 mM);10% DMSO+40% PEG300+5% Tween 80+45% Saline:2 mg/mL (5.1 mM);H2O:< 1 mg/mL (insoluble or slightly soluble);DMSO:250 mg/mL (637.14 mM)

Bioactivity

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Target IC50	PknB:8 μM\|JAK1:11 nM (Ki)\|JAK2:13 nM (Ki)\|FLT3:1 μM (Ki)\|Tyk2:11 nM (Ki)\|JAK3:2.5 nM(Ki)\|CDK2-CyclinA:2.6 μM (Ki)\|GSK-3β:1.8 μM (Ki)\|ROCK1:1.5 μM (Ki)
In Vivo	In a rat model of collagen-induced arthritis, Decernotinib(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, Decernotinib(50 mg/kg, p.o.) significantly suppresses ear edema. In a rat HvG model, Decernotinib(50 mg/kg, p.o.) results in dose-dependent inhibition of popletial lymph node (PLN) hyperplasia. Read more...
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. Read more...
Cell Research	Frozen purified human B cells atr thawed, washed, and resuspended in complete medium. Cells are plated onto a 96-well plate at a density of 2 × 105 cells/well. VX-509 is added, and plates are incubated for 30 minutes at 37°C, followed by stimulation with a combination of 10 ng/ml IL-4 and 1 μg/ml CD40L. DMSO alone is added to the top two rows, one of which is stimulated with IL-4 or CD40L (negative control) and the other of which served as a proliferation control. The plates are incubated at 37°C for 6 days. On day 6, cells are pulsed with [3H]thymidine for 7 hours and harvested onto filters for radioactive determination using a PerkinElmer-Wallace beta counter (1205 Betaplate Beta Liquid Scintillation Counter). Data are analyzed with Softmax pro software to generate an IC50 value.(Only for Reference) Read more...

Storage & Handling

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Storage	Powder: -20°C for 3 years \| In solvent: -80°C for 1 year \| Shipping with blue ice/Shipping at ambient temperature.
Expiration Date	12 months from date of receipt.
Disclaimer	For research use only

Alternative Names

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inhibit, JAK3, Janus kinase, JAK1, JAK2, JAK, Inhibitor, Decernotinib, VX 509, VX509, VX-509, VRT831509, VRT-831509, VRT 831509, TyrosineKinases, Tyrosine Kinases, Tyk2

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Compound Identifiers

PubChem CID

59422203 ↗

Key Properties

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No computed properties available.

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Purity:	>98% (HPLC)
CAS Number:	944842-54-0
MW:	392.4
Formula:	C₁₈H₁₉F₃N₆O

Decernotinib

Description

Research Area

Images & Validation

Key Properties

Bioactivity

Storage & Handling

Alternative Names

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