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Decernotinib

Catalog No. T2636   CAS 944842-54-0
Synonyms: VX-509, VRT-831509

Decernotinib (VRT-831509)(VX-509; VRT-831509) is a potent and selective Janus kinase 3 (JAK3) inhibitor with Ki of 2.5 nM; IC50 is 50-170 nM in cellular assays.

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Decernotinib Chemical Structure
Decernotinib, CAS 944842-54-0
Pack Size Availability Price/USD Quantity
1 mg In stock $ 44.00
2 mg In stock $ 63.00
5 mg In stock $ 96.00
10 mg In stock $ 135.00
25 mg In stock $ 275.00
50 mg In stock $ 489.00
100 mg In stock $ 688.00
500 mg In stock $ 1,430.00
1 mL * 10 mM (in DMSO) In stock $ 81.00
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Purity: 100%
Purity: 99.64%
Purity: 99.45%
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Biological Description
Chemical Properties
Storage & Solubility Information
Description Decernotinib (VRT-831509)(VX-509; VRT-831509) is a potent and selective Janus kinase 3 (JAK3) inhibitor with Ki of 2.5 nM; IC50 is 50-170 nM in cellular assays.
Targets&IC50 JAK3:2.5 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. [1]
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. [1] In a rat HvG model, VX-509 (50 mg/kg, p.o.) results in dose-dependent inhibition of popletial lymph node (PLN) hyperplasia. [2]
Kinase Assay Kinase Activity Assays: The effect of VX-509 on JAK3 activity is assessed by measuring the residual kinase activity of the recombinantly expressed JAK3 kinase domain using a radiometric assay. The final concentrations of the components in the assay are as follows: 100 mM HEPES (pH 7.5), 10 mM MgCl2, 1 mM dithiothreitol (DTT), 0.01% BSA, 0.25 nM JAK3, 0.25 mg/ml polyE4Y, and 5 μM 33P-γ-ATP (200 μCi/μMol). A 10 mM stock solution of VX-509 is prepared in DMSO, from which additional dilutions are prepared. A substrate mixture (100 mM HEPES, 10 mM MgCl2, 0.5 mg/ml polyE4Y, and 10 μM 33P-γ-ATP) is added and mixed with VX-509 stock solution. The reaction is initiated by the addition of an enzyme mixture [100 mM HEPES (pH 7.5), 10 mM MgCl2, 2 mM DTT, 0.02% BSA, 0.5 nM JAK3]. After 15 minutes, the reaction was quenched with 20% trichloroacetic acid (TCA). The quenched reaction was transferred to the GF/B filter plates and washed three times with 5% TCA. Following the addition of Ultimate Gold scintillant (50 μl), the samples were counted in a Packard TopCount gamma counter (PerkinElmer). In this procedure, the radioactivity trapped is a measure of the residual JAK3 kinase activity. From the activity versus concentration of VX-509 titration curve, the Ki value was determined by fitting the data to an equation for competitive tight binding inhibition kinetics using Prism software.
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)
Synonyms VX-509, VRT-831509
Molecular Weight 392.38
Formula C18H19F3N6O
CAS No. 944842-54-0

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

H2O: < 1 mg/mL (insoluble or slightly soluble)

DMSO: 72 mg/mL (183.5 mM)

Ethanol: 16 mg/mL (40.8 mM)

TargetMolReferences and Literature

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.

Related compound libraries

This product is contained In the following compound libraries:
Tyrosine Kinase Inhibitor Library Anti-Cancer Drug Library Anti-Cancer Clinical Compound Library Orally Active Compound Library Anti-Pancreatic Cancer Compound Library JAK-STAT Compound Library Anti-Obesity Compound Library Apoptosis Compound Library Clinical Compound Library Anti-Prostate Cancer Compound Library

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Keywords

Decernotinib 944842-54-0 Angiogenesis Chromatin/Epigenetic JAK/STAT signaling Stem Cells Tyrosine Kinase/Adaptors Tyrosine Kinases JAK VX509 VX-509 VRT831509 inhibit VRT-831509 Janus kinase VX 509 VRT 831509 Inhibitor inhibitor

 

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