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SAR-20347

Catalog No. T4210   CAS 1450881-55-6
Synonyms: SAR20347

SAR-20347 is an inhibitor of TYK2, JAK1/2/3 (IC50: 0.6/23/26/41 nM).

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SAR-20347 Chemical Structure
SAR-20347, CAS 1450881-55-6
Pack Size Availability Price/USD Quantity
1 mg In stock $ 34.00
2 mg In stock $ 48.00
5 mg In stock $ 80.00
10 mg In stock $ 147.00
25 mg In stock $ 322.00
50 mg In stock $ 578.00
100 mg In stock $ 833.00
500 mg In stock $ 1,690.00
1 mL * 10 mM (in DMSO) In stock $ 89.00
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Purity: 99.77%
Purity: 99.54%
Purity: 99.35%
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Biological Description
Chemical Properties
Storage & Solubility Information
Description SAR-20347 is an inhibitor of TYK2, JAK1/2/3 (IC50: 0.6/23/26/41 nM).
Targets&IC50 JAK2:26nM, JAK1:23nM, TYK2:0.6 nM, JAK3:41 nM
In vitro SAR-20347 effectively inhibits IL-12-mediated STAT4 phosphorylation (TYK2-dependent, IC50: 126 nM) when NK-92 cells are stimulated with IL-12. In the culture media, cells without IL-12 have no measurable IFN-γ, while cells incubated with IL-12 and SAR-20347 demonstrate dose-dependent inhibition of IFN-γ production. SAR-20347 (maximum effect: 5 μM) dose-dependently inhibits the production of secreted embryonic alkaline phosphatase (SEAP).
In vivo Compared to vehicle-treated animals, SAR-20347 (60 mg/kg) inhibits the production of IFN-γ in the serum by 91%, demonstrating that SAR-20347 can inhibit TYK2 signaling in vivo. SAR-20347 markedly reduces IL-17 production as measured by average signal intensity, consistent with the gene expression analysis.
Kinase Assay 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].
Cell Research 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)[1].
Animal Research 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. On the 6th day, the animals are euthanized and photographs are taken[1].
Synonyms SAR20347
Molecular Weight 444.84
Formula C21H18ClFN4O4
CAS No. 1450881-55-6

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 100 mg/mL

TargetMolReferences and Literature

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. 2. Kang X, Yang M, Shi Y, et al. Interleukin-15 facilitates muscle regeneration through modulation of fibro/adipogenic progenitors[J]. Cell Communication and Signaling. 2018 Jul 20;16(1):42.

TargetMolCitations

1. Kang X, Yang M, Shi Y, et al. Interleukin-15 facilitates muscle regeneration through modulation of fibro/adipogenic progenitors. Cell Communication and Signaling. 2018 Jul 20;16(1):42 2. Zhang X, Wang J, Wang M, et al.IFN-β Pretreatment Alleviates Allogeneic Renal Tubular Epithelial Cell–Induced NK Cell Responses via the IRF7/HLA-E/NKG2A Axis.The Journal of Immunology.2023

Related compound libraries

This product is contained In the following compound libraries:
Tyrosine Kinase Inhibitor Library Kinase Inhibitor Library Inhibitor Library Anti-Pancreatic Cancer Compound Library Stem Cell Differentiation Compound Library Anti-Liver Cancer Compound Library Anti-Lung Cancer Compound Library Hematonosis Compound Library Bioactive Compounds Library Max Bioactive Compound Library

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Keywords

SAR-20347 1450881-55-6 Angiogenesis Chromatin/Epigenetic JAK/STAT signaling Stem Cells Tyrosine Kinase/Adaptors Tyrosine Kinases JAK inhibit Janus kinase SAR20347 SAR 20347 Inhibitor inhibitor

 

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