Decernotinib
Based on 4 publication(s) in Google Scholar
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.
商品は「研究用試薬」です。人や動物の医療用・臨床診断用・食品用の製品ではありません。
研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- 純度 : 99.91%
- CAS 番号: 944842-54-0
- 分子式: C18H19F3N6O
- 分子量:392.38
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保管条件:
4°C, protect from light, stored under nitrogen
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen)
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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生物活性
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化学情報
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溶剤 & 溶解度
- 純度とドキュメンテーション
- 参考文献
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Help & FAQs
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MedChemExpress（MCE）の使用を引用している文献 Decernotinib
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生物活性
製品説明
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) |
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| B cell | IC50 |
50 nM
Compound: 48
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Inhibition of cell proliferation in CD40L/IL-4-induced human B cells
Inhibition of cell proliferation in CD40L/IL-4-induced human B cells
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[PMID: 32120325] |
| HEL | IC50 |
2.56 μM
Compound: Decernotinib
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Cytotoxicity against HEL cells assessed as inhibition of cell growth
Cytotoxicity against HEL cells assessed as inhibition of cell growth
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[PMID: 36805946] |
| Splenocyte | IC50 |
50 nM
Compound: 48
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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
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[PMID: 32120325] |
| Splenocyte | IC50 |
50 nM
Compound: 48
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Inhibition of T cell proliferation in CBA mouse spleenocytes by MLR assay
Inhibition of T cell proliferation in CBA mouse spleenocytes by MLR assay
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[PMID: 32120325] |
| T-cell | IC50 |
50 nM
Compound: 48
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Inhibition of IL-2 stimulated human T cell proliferation
Inhibition of IL-2 stimulated human T cell proliferation
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[PMID: 32120325] |
体外実験
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].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. .
体内実験
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
臨床実験
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
化学情報
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CAS 番号 944842-54-0
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性状 Solid
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分子量 392.38
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分子式 C18H19F3N6O
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Color White to off-white
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SMILES
C[C@](C(NCC(F)(F)F)=O)(CC)NC1=NC(C2=CNC3=NC=CC=C32)=NC=C1
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別名
VX-509; VRT-831509
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
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
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Most Recent
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Science
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
2020 Oct 15:24:100832. PMID: 33102814
溶剤 & 溶解度
体外:
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.
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.
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.
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
体内:
Select the appropriate dissolution method based on your experimental animal and administration route.
- 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.
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.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
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.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%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
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL. * In solvent : -80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen)
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
純度とドキュメンテーション
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データシート (282 KB)
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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)
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取扱説明書 (2659 KB)
参考文献
Complete Stock Solution Preparation Table
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.
| 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 |
Decernotinib 関連分類
HY-12469 関連分類
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