SAR-20347
Based on 2 publication(s) in Google Scholar
SAR-20347 is an inhibitor of TYK2, JAK1, JAK2 and JAK3 with IC50s of 0.6, 23, 26 and 41 nM, respectively.
Para uso exclusivo en investigación. No vendemos a pacientes.
- Pureza : 97.27%
- No. CAS: 1450881-55-6
- Fòrmula: C21H18ClFN4O4
- Peso molecular:444.84
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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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Publications Citing Use of MedChemExpress (MCE) SAR-20347
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Actividad biológica
Descripciòn
IC50 & Target
[1]|
Tyk2 0.6 nM (IC50) |
JAK1 23 nM (IC50) |
JAK2 26 nM (IC50) |
JAK3 41 nM (IC50) |
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| Jurkat | IC50 |
0.6 nM
Compound: SAR-20347
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Inhibition of TYK2 in human Jurkat cells assessed as reduction in IFN-alpha stimulated TYK2 phosphorylation by caspase3/7 reagent-based Western blot analysis
Inhibition of TYK2 in human Jurkat cells assessed as reduction in IFN-alpha stimulated TYK2 phosphorylation by caspase3/7 reagent-based Western blot analysis
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[PMID: 30530193] |
| Jurkat | IC50 |
23 nM
Compound: SAR-20347
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Inhibition of JAK1 in human Jurkat cells assessed as reduction in IFN-alpha stimulated JAK1 phosphorylation by caspase3/7 reagent-based Western blot analysis
Inhibition of JAK1 in human Jurkat cells assessed as reduction in IFN-alpha stimulated JAK1 phosphorylation by caspase3/7 reagent-based Western blot analysis
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[PMID: 30530193] |
| Jurkat | IC50 |
26 nM
Compound: SAR-20347
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Inhibition of JAK2 in human Jurkat cells assessed as reduction in IFN-alpha stimulated JAK2 phosphorylation by caspase3/7 reagent-based Western blot analysis
Inhibition of JAK2 in human Jurkat cells assessed as reduction in IFN-alpha stimulated JAK2 phosphorylation by caspase3/7 reagent-based Western blot analysis
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[PMID: 30530193] |
| Jurkat | IC50 |
41 nM
Compound: SAR-20347
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Inhibition of JAK3 in human Jurkat cells assessed as reduction in IFN-alpha stimulated JAK3 phosphorylation by caspase3/7 reagent-based Western blot analysis
Inhibition of JAK3 in human Jurkat cells assessed as reduction in IFN-alpha stimulated JAK3 phosphorylation by caspase3/7 reagent-based Western blot analysis
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[PMID: 30530193] |
In Vitro
When NK-92 cells are stimulated with IL-12, SAR-20347 potently inhibits IL-12-mediated STAT4 phosphorylation, a TYK2-dependent event, with an IC50 of 126 nM. SAR-20347 demonstrates a selectivity of TYK2>JAK1>JAK2>JAK3. Cells without IL-12 in the culture media have no measureable IFN-γ, while cells incubated with IL-12 and SAR-20347 demonstrate dose-dependent inhibition of IFN-γ production. SAR-20347 dose-dependently inhibits the production of secreted embryonic alkaline phosphatase (SEAP) with greatest inhibition occurring with 5 μM of SAR-20347 in these experiments[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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No. CAS 1450881-55-6
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Appearance Solid
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Peso molecular 444.84
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Fòrmula C21H18ClFN4O4
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Color Light yellow to yellow
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SMILES
O=C(C1=C(NC2=CC=C(C(N3CCOCC3)=O)C=C2)OC(C4=C(F)C=CC=C4Cl)=N1)N
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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
Publications (2)
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Journal Impact Factor
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Most Recent
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Cancer Cell
Activated T cell extracellular vesicle DNA transfer enhances antigen presentation and anti-tumor immunity. [Abstract]2026 May 11;44(5):965-982.e12. PMID: 42066762 -
Cell Res
Virus-induced accumulation of intracellular bile acids activates the TGR5-β-arrestin-SRC axis to enable innate antiviral immunity. [Abstract]2019 Mar;29(3):193-205. PMID: 30651583
Solvente y solubilidad
In Vitro:
DMSO : 100 mg/mL (224.80 mM; Need ultrasonic and warming; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
H2O : < 0.1 mg/mL (insoluble)
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: ≥ 2.5 mg/mL (5.62 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 (5.62 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.
Protocolo
Kinase Assay[1]
Kinases are prepared in Base Reaction Buffer (20 mM Hepes pH 7.5, 10 mM MgCl2, 1 mM EGTA, 0.02% Brij35, 0.02 mg/mL BSA, 0.1 mM Na3VO4, 2 mM DTT, 1% DMSO) and substrate is added with 1.5 mM CaCl2, 16 μg/mL Calmodulin, and 2 mM MnCl2. Varying concentrations of SAR-20347 in DMSO are added to the kinase reaction along with 10 μM 33P-ATP (activity 0.01 μCi/μL final) for IC50 determination[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Cell Assay[1]
Cells are plated in a 96-well v-bottom plate in starvation medium, incubated with SAR-20347 (0.5% DMSO) for 20 minutes at 37°C, 5% CO2, and stimulated with individual cytokines. P-STAT levels are measured in duplicate using MSD plates following the manufacturer's instructions (MSD). The IC50 is determined by subtracting background (no cytokine) and relative to DMSO/cytokine control[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Administration[1]
Female 7 to 9 week old C57BL/6 mice are used. Mice are administered vehicle or 50 mg/kg SAR-20347 by oral gavage 30 minutes prior to application of 62.5 mg 5% imiquimod cream or control cream. Another dose of vehicle or 50 mg/kg SAR-20347 is given 5.5 hours following the first dose. This treatment is repeated for 5 days and on day 3 and 4, animals are injected with 100 uL saline to prevent dehydration. Each day, the mice are assessed by the same researcher for redness. On the 6th day, the animals are euthanized and photographs are taken[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Pureza y Documentación
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Ficha de datos (281 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 | 2.2480 mL | 11.2400 mL | 22.4800 mL | 56.2000 mL |
| 5 mM | 0.4496 mL | 2.2480 mL | 4.4960 mL | 11.2400 mL | |
| 10 mM | 0.2248 mL | 1.1240 mL | 2.2480 mL | 5.6200 mL | |
| 15 mM | 0.1499 mL | 0.7493 mL | 1.4987 mL | 3.7467 mL | |
| 20 mM | 0.1124 mL | 0.5620 mL | 1.1240 mL | 2.8100 mL | |
| 25 mM | 0.0899 mL | 0.4496 mL | 0.8992 mL | 2.2480 mL | |
| 30 mM | 0.0749 mL | 0.3747 mL | 0.7493 mL | 1.8733 mL | |
| 40 mM | 0.0562 mL | 0.2810 mL | 0.5620 mL | 1.4050 mL | |
| 50 mM | 0.0450 mL | 0.2248 mL | 0.4496 mL | 1.1240 mL | |
| 60 mM | 0.0375 mL | 0.1873 mL | 0.3747 mL | 0.9367 mL | |
| 80 mM | 0.0281 mL | 0.1405 mL | 0.2810 mL | 0.7025 mL | |
| 100 mM | 0.0225 mL | 0.1124 mL | 0.2248 mL | 0.5620 mL |
SAR-20347 Related Classifications
HY-100895 Related Classifications
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