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Deucravacitinib

Catalog No. T14687   CAS 1609392-27-9
Synonyms: BMS-986165

Deucravacitinib (BMS-986165) inhibits IL-12/23 and type I IFN pathways[1][2]. BMS-986165 is a highly selective, orally bioavailable allosteric TYK2 inhibitor for the treatment of autoimmune diseases. Which selectively binds to TYK2 pseudokinase (JH2) domain (IC50=1.0 nM) and blocks receptor-mediated Tyk2 activation by stabilizing the regulatory JH2 domain.

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Deucravacitinib Chemical Structure
Deucravacitinib, CAS 1609392-27-9
Pack Size Availability Price/USD Quantity
1 mg In stock $ 64.00
5 mg In stock $ 155.00
10 mg In stock $ 289.00
25 mg In stock $ 455.00
50 mg In stock $ 672.00
100 mg In stock $ 956.00
200 mg In stock $ 1,290.00
500 mg In stock $ 1,920.00
1 mL * 10 mM (in DMSO) In stock $ 169.00
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Purity: 100%
Purity: 99.43%
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Biological Description
Chemical Properties
Storage & Solubility Information
Description Deucravacitinib (BMS-986165) inhibits IL-12/23 and type I IFN pathways[1][2]. BMS-986165 is a highly selective, orally bioavailable allosteric TYK2 inhibitor for the treatment of autoimmune diseases. Which selectively binds to TYK2 pseudokinase (JH2) domain (IC50=1.0 nM) and blocks receptor-mediated Tyk2 activation by stabilizing the regulatory JH2 domain.
Targets&IC50 JAK1 JH2:1 nM, Tyk2 JH2:0.2 nM
In vitro BMS-986165 maintains excellent potency in human and mouse whole blood (IC50s=13 and 100 nM, respectively). Which shows no significant hERG inhibition in the flux assay (IC50>80 μM).BMS-986165 is differentiated from previous JAK inhibitors due its unique ability to selectively bind to the pseudokinase (JH2) domain of TYK2 and inhibit its function through an allosteric mechanism[1].
In vivo BMS-986165 as a high affinity JH2 ligand and potent allosteric inhibitor of TYK2. In addition to unprecedented JAK isoform and kinome selectivity, BMS-986165 shows excellent pharmacokinetic properties with minimal profiling liabilities and is efficacious in several murine models of autoimmune disease. On the basis of these findings, BMS-986165 appears differentiated from all other reported JAK inhibitors and has been advanced as the first pseudokinase-directed therapeutic in clinical development as an oral treatment for autoimmune diseases[1].
Synonyms BMS-986165
Molecular Weight 425.46
Formula C20H19D3N8O3
CAS No. 1609392-27-9

Storage

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

Solubility Information

DMSO: 32.5mg/ml (76.39 Mm), sonification is recommended.

TargetMolReferences and Literature

1. Wrobleski ST, et al. Highly Selective Inhibition of Tyrosine Kinase 2 (TYK2) for the Treatment of Autoimmune Diseases: Discovery of the Allosteric Inhibitor BMS-986165. J Med Chem. 2019 Jul 18. 2. Catlett I, et al. SAT0226 A first-in-human, study of BMS-986165, a selective, potent, allosteric small molecule inhibitor of tyrosine kinase 2. Annals of the Rheumatic Diseases 2017;76:859.

Related compound libraries

This product is contained In the following compound libraries:
Tyrosine Kinase Inhibitor Library Highly Selective Inhibitor Library Anti-Cancer Drug Library Anti-Cancer Approved Drug Library Anti-Cancer Clinical Compound Library Stem Cell Differentiation Compound Library Bioactive Compound Library Epigenetics Compound Library Reprogramming Compound Library Immunology/Inflammation Compound Library

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Keywords

Deucravacitinib 1609392-27-9 Angiogenesis Chromatin/Epigenetic Immunology/Inflammation JAK/STAT signaling Stem Cells Tyrosine Kinase/Adaptors Tyrosine Kinases JAK IFNAR Interleukin Janus kinase inhibit Interleukin Related Interferon-alpha/beta receptor Interferon-α/β receptor Inhibitor BMS 986165 BMS986165 BMS-986165 inhibitor

 

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