TCS 21311
Based on 1 Customer Validation
TCS 21311 (NIBR3049) is a potent, highly selective JAK3 inhibitor with an IC50 of 8 nM, it displays >100-fold selectivity over JAK1, JAK2 and TYK2. TCS 21311 (NIBR3049) inhibits PKCα, PKCθ, and GSK3β with IC50s of 13, 68, and 3 nM, respectively.
Para uso exclusivo en investigación. No vendemos a pacientes.
- Pureza: 99.49%
- No. CAS: 1260181-14-3
- Fòrmula: C27H25F3N4O4
- Peso molecular:526.51
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Almacenamiento:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
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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Actividad biológica
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Chemical Information
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Solvente y solubilidad
- Pureza y Documentación
- Referencias
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Help & FAQs
Actividad biológica
Descripciòn
IC50 & Target
[1]|
JAK3 8 nM (IC50) |
JAK2 2.55 μM (IC50) |
JAK1 1.017 μM (IC50) |
PKCα 13 nM (IC50) |
PKCθ 68 nM (IC50) |
GSK-3β 3 nM (IC50) |
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| CTLL | IC50 |
1294 nM
Compound: 1
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Inhibition of Jak3-mediated IL2-induced Stat5 phosphorylation in mouse CTLL cells by cell-based assay
Inhibition of Jak3-mediated IL2-induced Stat5 phosphorylation in mouse CTLL cells by cell-based assay
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[PMID: 21155605] |
| Jurkat | IC50 |
689 nM
Compound: 1
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Inhibition of antiTCR/antiCD28-stimulated IL2 production in human Jurkat cells by measuring bioluminescence
Inhibition of antiTCR/antiCD28-stimulated IL2 production in human Jurkat cells by measuring bioluminescence
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[PMID: 21155605] |
In Vitro
TCS 21311 (NIBR3049) exhibits IC50 values of 1.017, 2.550 and 8.055 μM for JAK1, JAK2 and TYK2, respectively in a enzymatic Jak assay[1]. TCS 21311 (NIBR3049) shows moderate activity in this cellular assay (IC50=689 nM, Jurkat cells), which is in good agreement with its enzymatic Pkc activity[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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No. CAS 1260181-14-3
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Appearance Solid
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Peso molecular 526.51
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Fòrmula C27H25F3N4O4
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Color White to yellow
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SMILES
O=C(C(C1=CC(N2CCN(C(C(C)(O)C)=O)CC2)=CC=C1C(F)(F)F)=C3C4=CNC5=C4C=CC=C5)NC3=O
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Synonyms
NIBR3049
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Solvente y solubilidad
In Vitro:
DMSO : 100 mg/mL (189.93 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, 6 months; -20°C, 1 month. 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. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
In Vivo:
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 (4.75 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 (4.75 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.
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.
Pureza y Documentación
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Ficha de datos (280 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
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Instrucciones de manejo (2659 KB)
Referencias
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. 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 | 1.8993 mL | 9.4965 mL | 18.9930 mL | 47.4825 mL |
| 5 mM | 0.3799 mL | 1.8993 mL | 3.7986 mL | 9.4965 mL | |
| 10 mM | 0.1899 mL | 0.9496 mL | 1.8993 mL | 4.7482 mL | |
| 15 mM | 0.1266 mL | 0.6331 mL | 1.2662 mL | 3.1655 mL | |
| 20 mM | 0.0950 mL | 0.4748 mL | 0.9496 mL | 2.3741 mL | |
| 25 mM | 0.0760 mL | 0.3799 mL | 0.7597 mL | 1.8993 mL | |
| 30 mM | 0.0633 mL | 0.3165 mL | 0.6331 mL | 1.5827 mL | |
| 40 mM | 0.0475 mL | 0.2374 mL | 0.4748 mL | 1.1871 mL | |
| 50 mM | 0.0380 mL | 0.1899 mL | 0.3799 mL | 0.9496 mL | |
| 60 mM | 0.0317 mL | 0.1583 mL | 0.3165 mL | 0.7914 mL | |
| 80 mM | 0.0237 mL | 0.1187 mL | 0.2374 mL | 0.5935 mL | |
| 100 mM | 0.0190 mL | 0.0950 mL | 0.1899 mL | 0.4748 mL |
TCS 21311 Related Classifications
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