Art. -Nr.: HY-12469

Decernotinib

(Synonyms: VX-509; VRT-831509)

4 Cited Publications

Kundenbewertung

Based on 4 publication(s) in Google Scholar

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

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Reinheit: 99.91%
CAS. Nr.: 944842-54-0
Formel: C₁₈H₁₉F₃N₆O
Molecular Weight:392.38

Speicherung:

4°C, protect from light, stored under nitrogen

* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen)

Decernotinib Chemical Structure

CAS. Nr.: 944842-54-0

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Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
- Clinical Trial
Chemical Information
Publications (4)
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Protokoll
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

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

IC₅₀ & Target^[1]

JAK3

2.5 nM (Ki)

JAK1

11 nM (Ki)

Tyk2

11 nM (Ki)

JAK2

13 nM (Ki)

FLT3

1 μM (Ki)

ROCK I

1.5 μM (Ki)

GSK3β

1.8 μM (Ki)

CDK2/CycA

2.6 μM (Ki)

PknB

8 μM (IC₅₀)

Alle JAK Isoform-spezifische Produkte anzeigen :

Cellular Effect

Cell Line	Type	Value	Description	References
B cell	IC₅₀	50 nM Compound: 48	Inhibition of cell proliferation in CD40L/IL-4-induced human B cells Inhibition of cell proliferation in CD40L/IL-4-induced human B cells	[PMID: 32120325]
HEL	IC₅₀	2.56 μM Compound: Decernotinib	Cytotoxicity against HEL cells assessed as inhibition of cell growth Cytotoxicity against HEL cells assessed as inhibition of cell growth	[PMID: 36805946]
Splenocyte	IC₅₀	50 nM Compound: 48	Inhibition of T cell proliferation in Balb/c mouse spleenocytes by MLR assay Inhibition of T cell proliferation in Balb/c mouse spleenocytes by MLR assay	[PMID: 32120325]
Splenocyte	IC₅₀	50 nM Compound: 48	Inhibition of T cell proliferation in CBA mouse spleenocytes by MLR assay Inhibition of T cell proliferation in CBA mouse spleenocytes by MLR assay	[PMID: 32120325]
T-cell	IC₅₀	50 nM Compound: 48	Inhibition of IL-2 stimulated human T cell proliferation Inhibition of IL-2 stimulated human T cell proliferation	[PMID: 32120325]

In Vitro

Decernotinib (VX-509) is a potent JAK3 inhibitor, with K_is 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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Clinical Trial

NCT Number	Sponsor	Condition	Start Date	Phase A549
NCT01329991	Plexxikon\|		2011-05	PHASE1

Chemical Information

CAS. Nr. 944842-54-0
Appearance Solid
Molecular Weight 392.38
Formel C₁₈H₁₉F₃N₆O
Color White to off-white
SMILES

C[C@](C(NCC(F)(F)F)=O)(CC)NC1=NC(C2=CNC3=NC=CC=C32)=NC=C1
Synonyms

VX-509; VRT-831509
Versand

Room temperature in continental US; may vary elsewhere.
Speicherung

4°C, protect from light, stored under nitrogen

* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen)

Publications (4)

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Journal Impact Factor

Science

The target landscape of clinical kinase drugs. [Abstract]

2017 Dec 1;358(6367):eaan4368. PMID: 29191878
Biochem Pharmacol

Dual inhibition of EGR1/STAT3 transcriptional hubs suppresses macrophage-driven liver fibrosis: A multi-omics-guided drug repurposing strategy. [Abstract]

2025 Oct:240:117120. PMID: 40623460
J Nat Prod

Discovering the Mechanisms of Wikstroelide E as a Potential HIV-Latency-Reversing Agent by Transcriptome Profiling. [Abstract]

2021 Apr 23;84(4):1022-1033. PMID: 33721994
Biochem Biophys Rep

Cucurbitacin E and I target the JAK/STAT pathway and induce apoptosis in Sézary cells. [Abstract]

2020 Oct 15:24:100832. PMID: 33102814

Lösungsmittel & Löslichkeit

In Vitro:

DMSO : ≥ 50 mg/mL (127.43 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

* "≥" means soluble, but saturation unknown.

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

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

Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.

Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Molaritätsrechner

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline

Solubility: ≥ 2.5 mg/mL (6.37 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

Protocol 2

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)

Solubility: ≥ 2.5 mg/mL (6.37 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: ≥ 2.5 mg/mL (6.37 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Working solution concentration: 0.22 mg/mL

Protokoll

Kinase Assay^[1]

The effect of Decernotinib 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 Decernotinib 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 Decernotinib 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 is quenched with 20% trichloroacetic acid (TCA). The quenched reaction is 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 are counted in a Packard TopCount gamma counter. In this procedure, the radioactivity trapped is a measure of the residual JAK3 kinase activity. From the activity versus concentration of Decernotinib titration curve, the K_i value is determined by fitting the data to an equation for competitive tight binding inhibition kinetics^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Assay^[1]

Whole-blood samples from healthy volunteers are used to collect peripheral blood mononuclear cells, which are plated in T75 tissue culture flasks at a density of 1 × 10⁶/mL. Cells are stimulated with 10 μg/mL phytohemagglutinin at 37°C for 72 hours. After 72 hours, cells are detached from the flask by scraping, washed, and plated at a density of 1 × 10⁵/well in a 96-well plate. Decernotinib (9.7 nM to 10 μM) is added, and plates are incubated for 30 minutes at 37°C, followed by stimulation with human IL-2. In two rows, only DMSO is added; one row is not stimulated with IL-2, and one row is stimulated with IL-2 to serve as the proliferation control. Plates are incubated at 37°C for 2 days. On day 2, cells are pulsed with 20 µCi/mL methyl-[³H]thymidine for 18-24 hours and harvested onto filters for radiographic determination. Data are analyzed to generate an IC₅₀ value using Softmax pro software^[1]

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Administration^[1]

Rat^[1]
The collagen-induced arthritis (CIA) rat model is used to evaluate the effects of oral Decernotinib [10 mg/kg b.i.d., 25 mg/kg b.i.d., 50 mg/kg b.i.d., 50 mg/kg q.d., or 100 mg/kg q.d.] on joint inflammation and histopathology. Female Lewis rats (157-187 g) are anesthetized with isoflurane and injected with 300 µL Freund’s incomplete adjuvant, containing 2 mg/mL bovine type II collagen, at the base of the tail and two sites on the back on days 0 and 6. The rats are randomized to study groups at the onset of paw swelling (arthritis), which occurs between days 10 and 11. Dosing of either Decernotinib or vehicle via oral gavage is initiated on the first day of established arthritis and continued to day 6 of arthritis. Dosing volume is 5 mL/kg. Groups are controls (no collagen injection plus vehicle; n = 4), collagen plus vehicle (n = 5), collagen plus Decernotinib 10 mg/kg b.i.d. (n = 8); collagen plus Decernotinib 10 mg/kg b.i.d. (n = 8); collagen plus (n = 8); collagen plus (n = 8); collagen plus (n = 8); collagen plu (n = 8); and collagen plus (n = 8); collagen plu (n = 8); all treatments are administered for 6 days. An additional group of rats is given collagen plus 10 mg/kg subcutaneous etanercept, a human tumor necrosis factor-α antagonist, on study days 11 and 14. Caliper measurements of normal (baseline) ankle joints begin on day 9 and continue through the last day of study. Differences in mean ankle diameter are tested for significance using Student’s t test, with significance set at P ≤ 0.05. The rats are euthanized on day 7 of arthritis, which is study day 17 or 18 depending on when animals are randomized to groups; paws and knees are harvested to determine paw weight and to conduct a histopathological analysis of inflammation (knee and ankle), pannus formation (ankle), cartilage destruction (knee), and bone resorption (knee and ankle). Scores range from 0 (normal) to 5 (severe pathology) and are assigned by a veterinary pathologist. Percent inhibition is calculated using the following formula: [(mean of treatment group) − (mean of control)] ÷ [(mean of collagen + vehicle) − (mean of control)]. Kruskal-Wallis one-way analysis of variance nonparametric tests are used to determine statistical significance among the histopathology groups, with significance set at P ≤ 0.05^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (282 KB)
SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[1]. Mahajan S, et al. VX-509 is a potent and selective Janus kinase 3 (JAK3) inhibitor that attenuates inflammation in animal models of autoimmune disease. J Pharmacol Exp Ther. 2015 Mar 11. pii: jpet.114.221176. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	2.5485 mL	12.7427 mL	25.4855 mL	63.7137 mL
	5 mM	0.5097 mL	2.5485 mL	5.0971 mL	12.7427 mL
	10 mM	0.2549 mL	1.2743 mL	2.5485 mL	6.3714 mL
	15 mM	0.1699 mL	0.8495 mL	1.6990 mL	4.2476 mL
	20 mM	0.1274 mL	0.6371 mL	1.2743 mL	3.1857 mL
	25 mM	0.1019 mL	0.5097 mL	1.0194 mL	2.5485 mL
	30 mM	0.0850 mL	0.4248 mL	0.8495 mL	2.1238 mL
	40 mM	0.0637 mL	0.3186 mL	0.6371 mL	1.5928 mL
	50 mM	0.0510 mL	0.2549 mL	0.5097 mL	1.2743 mL
	60 mM	0.0425 mL	0.2124 mL	0.4248 mL	1.0619 mL
	80 mM	0.0319 mL	0.1593 mL	0.3186 mL	0.7964 mL
	100 mM	0.0255 mL	0.1274 mL	0.2549 mL	0.6371 mL

Keywords

Decernotinib

4 Cited Publications

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Decernotinib

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Publications Citing Use of MedChemExpress (MCE) Decernotinib

Alle JAK Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Publications (4)

Lösungsmittel & Löslichkeit

Protokoll

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

Decernotinib Related Classifications

HY-12469 Related Classifications