Art. -Nr.: HY-100895

SAR-20347

2 Cited Publications

Kundenbewertung

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.

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Reinheit: 97.27%
CAS. Nr.: 1450881-55-6
Formel: C₂₁H₁₈ClFN₄O₄
Molecular Weight:444.84

Speicherung:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year

SAR-20347 Chemical Structure

CAS. Nr.: 1450881-55-6

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Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
Chemical Information
Publications (2)
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Protokoll
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

SAR-20347 is an inhibitor of TYK2, JAK1, JAK2 and JAK3 with IC₅₀s of 0.6, 23, 26 and 41 nM, respectively.

IC₅₀ & Target^[1]

Tyk2

0.6 nM (IC₅₀)

JAK1

23 nM (IC₅₀)

JAK2

26 nM (IC₅₀)

JAK3

41 nM (IC₅₀)

Alle JAK Isoform-spezifische Produkte anzeigen :

Cellular Effect

Cell Line	Type	Value	Description	References
Jurkat	IC₅₀	0.6 nM Compound: SAR-20347	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	[PMID: 30530193]
Jurkat	IC₅₀	23 nM Compound: SAR-20347	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	[PMID: 30530193]
Jurkat	IC₅₀	26 nM Compound: SAR-20347	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	[PMID: 30530193]
Jurkat	IC₅₀	41 nM Compound: SAR-20347	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	[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

60 mg/kg SAR-20347 inhibits the production of IFN-γ in the serum by 91% compare to vehicle-treated animals, demonstrating that SAR-20347 can inhibit TYK2 signaling in vivo. SAR-20347 treatment significantly reduces IL-17 production as measured by average signal intensity, consistent with the gene expression analysis^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Chemical Information

CAS. Nr. 1450881-55-6
Appearance Solid
Molecular Weight 444.84
Formel C₂₁H₁₈ClFN₄O₄
Color Light yellow to yellow
SMILES

O=C(C1=C(NC2=CC=C(C(N3CCOCC3)=O)C=C2)OC(C4=C(F)C=CC=C4Cl)=N1)N
Versand

Room temperature in continental US; may vary elsewhere.

Speicherung

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

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

Lösungsmittel & Löslichkeit

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)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

2.2480 mL

11.2400 mL

22.4800 mL

5 mM

0.4496 mL

2.2480 mL

4.4960 mL

10 mM

0.2248 mL

1.1240 mL

2.2480 mL

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.

Molaritätsrechner

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

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.

Protocol 1

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.

Protocol 2

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.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
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

Protokoll

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 6^th 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.

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (281 KB)
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)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[1]. Works MG, et al. Inhibition of TYK2 and JAK1 ameliorates imiquimod-induced psoriasis-like dermatitis by inhibiting IL-22 and the IL-23/IL-17 axis. J Immunol. 2014 Oct 1;193(7):3278-87. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

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

Keywords

SAR-20347

2 Cited Publications

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SAR-20347

Epigenetics Compound Library

Immunology/Inflammation Compound Library

JAK/STAT Compound Library

Kinase Inhibitor Library

Protein Tyrosine Kinase Compound Library

Stem Cell Signaling Compound Library

Anti-Cancer Compound Library

Anti-Aging Compound Library

Differentiation Inducing Compound Library

Reprogramming Compound Library

Anti-Breast Cancer Compound Library

Anti-Lung Cancer Compound Library

Anti-Pancreatic Cancer Compound Library

Anti-Blood Cancer Compound Library

Anti-Obesity Compound Library

Anti-Liver Cancer Compound Library

Anti-Prostate Cancer Compound Library

Cancer Stem Cells Compound Library

Heterocyclic Compound Library

Pain-Related Compound Library

Autoimmune Disease Compound Library

Highly Selective Inhibitors Library

Anti-Hematopathy Compound Library

Multi-Target Compound Library

Bioactive Compound Library Max

Epigenetics Compound Library Mini

MCE Bioactive Compound Library

Bioactive Compound Library

Protein Kinase Compound Library

High-Throughput Bioactive Compound Library

Anti-Rheumatic Arthritis Compound Library

Posttranslational Modification Library

Publications Citing Use of MedChemExpress (MCE) SAR-20347

Alle JAK Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Publications (2)

Lösungsmittel & Löslichkeit

Protokoll

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

SAR-20347 Related Classifications

HY-100895 Related Classifications