R112
Based on 1 Customer Validation
R112 is a fast and reversible inhibitor of spleen tyrosine kinase (Syk) kinase. R112 inhibits Syk kinase activity with an IC50 value of 226 nM and a Ki value of 96 nM. R112 inhibits IgE-FcεRI signaling pathway. R112 can be used for the research of allergic rhinitis.
Para uso exclusivo en investigación. No vendemos a pacientes.
- Pureza : 98.90%
- No. CAS: 575474-82-7
- Fòrmula: C16H13FN4O2
- Peso molecular:312.30
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Almacenamiento:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
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Actividad biológica
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Chemical Information
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Solvente y solubilidad
- Protocolo
- Pureza y Documentación
- Referencias
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Help & FAQs
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Actividad biológica
Descripciòn
IC50 & Target
IC50: 226 nM (Syk kinase)[1]
In Vitro
R112 (0.001-10 μM; 1 h) dose-dependently inhibits anti-IgE-mediated tryptase release and histamine release with EC50s of 0.353 and 0.28 μM, inhibits histamine release by basophils stimulated with an EC50 value of 0.49 μM, inhibits secretion of LTC4, TNF-α, GM-CSF and IL-8 with EC50s of 0.115, 2.01, 1.58 and 1.75 μM, respectively[1]. R112 (0-10 μM; 40 min) inhibits Syk target LAT (Y191) phosphorylation[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:Human mast cells
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Concentration:0.4, 2 and 10 μM
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Incubation Time:40 min
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Result:Inhibited phosphorylation of the Syk target LAT (Y191) and also inhibited phosphorylation of Syk downstream events.
Chemical Information
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No. CAS 575474-82-7
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Appearance Solid
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Peso molecular 312.30
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Fòrmula C16H13FN4O2
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Color Light yellow to yellow
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SMILES
FC1=CN=C(NC2=CC(O)=CC=C2)N=C1NC3=CC(O)=CC=C3
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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 2 years -20°C 1 year
Solvente y solubilidad
In Vitro:
DMSO : 55 mg/mL (176.11 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.
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: ≥ 2.75 mg/mL (8.81 mM); Clear solution
This protocol yields a clear solution of ≥ 2.75 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (27.5 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: ≥ 2.75 mg/mL (8.81 mM); Clear solution
This protocol yields a clear solution of ≥ 2.75 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (27.5 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 (271 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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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, 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 | 3.2020 mL | 16.0102 mL | 32.0205 mL | 80.0512 mL |
| 5 mM | 0.6404 mL | 3.2020 mL | 6.4041 mL | 16.0102 mL | |
| 10 mM | 0.3202 mL | 1.6010 mL | 3.2020 mL | 8.0051 mL | |
| 15 mM | 0.2135 mL | 1.0673 mL | 2.1347 mL | 5.3367 mL | |
| 20 mM | 0.1601 mL | 0.8005 mL | 1.6010 mL | 4.0026 mL | |
| 25 mM | 0.1281 mL | 0.6404 mL | 1.2808 mL | 3.2020 mL | |
| 30 mM | 0.1067 mL | 0.5337 mL | 1.0673 mL | 2.6684 mL | |
| 40 mM | 0.0801 mL | 0.4003 mL | 0.8005 mL | 2.0013 mL | |
| 50 mM | 0.0640 mL | 0.3202 mL | 0.6404 mL | 1.6010 mL | |
| 60 mM | 0.0534 mL | 0.2668 mL | 0.5337 mL | 1.3342 mL | |
| 80 mM | 0.0400 mL | 0.2001 mL | 0.4003 mL | 1.0006 mL | |
| 100 mM | 0.0320 mL | 0.1601 mL | 0.3202 mL | 0.8005 mL |
R112 Related Classifications
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