JAK3-IN-1
Based on 1 Customer Validation
JAK3-IN-1 is a potent, selective and orally active JAK3 inhibitor with an IC50 of 4.8 nM. JAK3-IN-1 shows over 180-fold more selective for JAK3 than JAK1 (IC50 of 896 nM) and JAK2 (IC50 of 1050 nM).
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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 : 99.31%
- CAS 番号: 1805787-93-2
- 分子式: C26H30ClN7O2
- 分子量:508.02
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保管条件:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
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
生物活性
製品説明
IC50 & Target
[1]|
JAK3 4.8 nM (IC50) |
JAK1 896 nM (IC50) |
JAK2 1050 nM (IC50) |
TTK 49 nM (IC50) |
BTK 794 nM (IC50) |
ITK 1070 nM (IC50) |
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| BaF3 | IC50 |
2266 nM
Compound: 9
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Antiproliferative activity against mouse BA/F3 cells expressing TYK2 E957D mutant after 72 hrs by cell titer glo assay
Antiproliferative activity against mouse BA/F3 cells expressing TYK2 E957D mutant after 72 hrs by cell titer glo assay
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[PMID: 26258521] |
| BaF3 | IC50 |
3047 nM
Compound: 9
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Antiproliferative activity against mouse BA/F3 cells expressing TEL-ABL after 72 hrs by cell titer glo assay
Antiproliferative activity against mouse BA/F3 cells expressing TEL-ABL after 72 hrs by cell titer glo assay
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[PMID: 26258521] |
| BaF3 | IC50 |
3124 nM
Compound: 9
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Antiproliferative activity against mouse BA/F3 cells expressing TEL-JAK1 after 72 hrs by cell titer glo assay
Antiproliferative activity against mouse BA/F3 cells expressing TEL-JAK1 after 72 hrs by cell titer glo assay
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[PMID: 26258521] |
| BaF3 | IC50 |
3194 nM
Compound: 9
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Antiproliferative activity against mouse BA/F3 cells expressing TEL-JAK2 after 72 hrs by cell titer glo assay
Antiproliferative activity against mouse BA/F3 cells expressing TEL-JAK2 after 72 hrs by cell titer glo assay
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[PMID: 26258521] |
| BaF3 | IC50 |
69 nM
Compound: 9
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Antiproliferative activity against mouse BA/F3 cells expressing TEL-JAK3 after 72 hrs by cell titer glo assay
Antiproliferative activity against mouse BA/F3 cells expressing TEL-JAK3 after 72 hrs by cell titer glo assay
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[PMID: 26258521] |
体外実験
JAK3-IN-1(Compound 9; 0-5 µM; 3 hours; BMDMs cells) treatment completely inhibits IL-4 induced p-STAT6 at a concentration of 500 nM and only partially inhibits IFNβ-induced p-STAT1 at a concentration of 5.0 μM[1].
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JAK3-IN-1(Compound 9) most potently inhibits JAK3 and identified fms-related tyrosine kinase 3 (FLT3) and several tyrosine protein kinase (TEC)-family kinases as being potential off-targets. Enzymatic assays using the Z’-lyte or LanthaScreen formats confirmed enzymatic inhibition of FLT3 (IC50 = 13 nM), TTK protein kinase (TTK, IC50 = 49 nM), BLK proto-oncogene (BLK, IC50 = 157 nM) and tyrosine protein kinase TXK (TXK, IC50 = 36 nM). JAK3-IN-1 shows very low inhibition scores for other JAKs and wild-type (WT) EGFR, which is consistent with the over 180-fold higher IC50s against EGFRWT and TYK2 (IC50s =409 nM, > 10000 respectively). JAK3-IN-1 possesses over 165-fold higher IC50s for BTK or ITK (IC50s = 794 and 1070 nM respectively)[1].
JAK3-IN-1(Compound 9) selectively inhibits the proliferation of JAK3-dependent Ba/F3 cells (IC50 = 69 nM) relative to other JAK-dependent Ba/F3 cells, for which there was no antiproliferative effect at concentrations below 3.0 μM[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:BMDMs cells
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Concentration:0 µM, 0.1 µM, 0.5 µM, 1 µM, 5 µM
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Incubation Time:3 hours
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Result:Completely inhibited IL-4 induced p-STAT6 at a concentration of 500 nM and only partially inhibited IFNβ-induced p-STAT1 at a concentration of 5.0 μM.
体内実験
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
化学情報
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CAS 番号 1805787-93-2
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性状 Solid
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分子量 508.02
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分子式 C26H30ClN7O2
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Color White to off-white
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SMILES
O=C(C=C)NC1=CC(CNC2=NC(NC3=C(OC)C=C(N4CCN(C)CC4)C=C3)=NC=C2Cl)=CC=C1
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
溶剤 & 溶解度
体外:
DMSO : 100 mg/mL (196.84 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
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 (4.92 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 (4.92 mM); Suspended solution; Need ultrasonic
This protocol yields a suspended solution of 2.5 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.
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.
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 (272 KB)
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SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 1.9684 mL | 9.8421 mL | 19.6843 mL | 49.2107 mL |
| 5 mM | 0.3937 mL | 1.9684 mL | 3.9369 mL | 9.8421 mL | |
| 10 mM | 0.1968 mL | 0.9842 mL | 1.9684 mL | 4.9211 mL | |
| 15 mM | 0.1312 mL | 0.6561 mL | 1.3123 mL | 3.2807 mL | |
| 20 mM | 0.0984 mL | 0.4921 mL | 0.9842 mL | 2.4605 mL | |
| 25 mM | 0.0787 mL | 0.3937 mL | 0.7874 mL | 1.9684 mL | |
| 30 mM | 0.0656 mL | 0.3281 mL | 0.6561 mL | 1.6404 mL | |
| 40 mM | 0.0492 mL | 0.2461 mL | 0.4921 mL | 1.2303 mL | |
| 50 mM | 0.0394 mL | 0.1968 mL | 0.3937 mL | 0.9842 mL | |
| 60 mM | 0.0328 mL | 0.1640 mL | 0.3281 mL | 0.8202 mL | |
| 80 mM | 0.0246 mL | 0.1230 mL | 0.2461 mL | 0.6151 mL | |
| 100 mM | 0.0197 mL | 0.0984 mL | 0.1968 mL | 0.4921 mL |
JAK3-IN-1 関連分類
HY-19544 関連分類
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