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Deucravacitinib

Catalog No. T14687 CAS 1609392-27-9

Synonyms: BMS-986165

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, CAS 1609392-27-9

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Purity: 98%

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Storage & Solubility Information

Description	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	Tyk2 JH2:0.2 nM, JAK1 JH2:1 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	C20H22N8O3
CAS No.	1609392-27-9

Storage

Powder: -20°C for 3 years

In solvent: -80°C for 2 years

Solubility Information

DMSO: 32.5mg/ml (76.39 Mm), Need ultrasonic

( < 1 mg/ml refers to the product slightly soluble or insoluble )

References 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：

Anti-Cancer Compound Library Anti-Pancreatic Cancer Compound Library Inhibitor Library Immunology/Inflammation Compound Library Drug Repurposing Compound Library Kinase Inhibitor Library Stem Cell Differentiation Compound Library Epigenetics Compound Library Angiogenesis related Compound Library JAK-STAT Compound Library

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Alpinone 3-acetate CCCP Vadimezan Cridanimod AX-024 hydrochloride Ginsenoside F3 RO8191 Deucravacitinib

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Keywords

Deucravacitinib 1609392-27-9 JAK/STAT信号通路表观遗传蛋白酪氨酸激酶干细胞免疫与炎症血管生成 IFNAR Interleukin JAK Tyrosine Kinases Janus kinase inhibit Interleukin Related Interferon-alpha/beta receptor BMS 986165 Interferon-α/β receptor BMS-986165 Inhibitor BMS986165 inhibitor

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