Home Protein Tyrosine Kinase JAK inhibitor - IFN inhibitor - Interleukins inhibitor Deucravacitinib (BMS-986165) For research use only.

Deucravacitinib (BMS-986165)

Deucravacitinib (BMS-986165) is a highly potent and selective allosteric inhibitor of Tyk2 with a Ki value of 0.02 nM for binding to the Tyk2 pseudokinase domain. It is highly selective against a panel of 265 kinases and pseudokinases.

Deucravacitinib (BMS-986165) Chemical Structure

Deucravacitinib (BMS-986165) Chemical Structure

CAS: 1609392-27-9

Selleck's Deucravacitinib (BMS-986165) has been cited by 4 publications

Purity & Quality Control

Batch: Purity: 99.9%
99.9

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Biological Activity

Description Deucravacitinib (BMS-986165) is a highly potent and selective allosteric inhibitor of Tyk2 with a Ki value of 0.02 nM for binding to the Tyk2 pseudokinase domain. It is highly selective against a panel of 265 kinases and pseudokinases.
Targets
Tyk2 [1]
(Cell-free assay)
0.02 nM
In vitro
In vitro

BMS-986165 is highly differentiated from all other reported JAK/TYK2 inhibitors due to its ability to achieve an unprecedented level of selectivity for TYK2, especially over JAK1, JAK2, and JAK3.[1]
Cell Research Cell lines CD3+ T-cells, CD161+ CD3+ T-cells, TF-1 cells, mononuclear cells, platelets
Concentrations 0 - 10 μM
Incubation Time --
Method

BMS-986165 is evaluated in both binding and human cellular assays to determine selectivity within the JAK family and across the kinome. Mean values are determined from at least three separate experiments unless otherwise noted. Measuring STAT5 phosphorylation in CD3+ T-cells as end point. Measuring STAT3 phosphorylation in CD161+ CD3+ T-cells. Measuring STAT5A phosphorylation in TF-1 cells (n = 2). Measuring STAT6 phosphorylation in mononuclear cells (n = 2). Measuring STAT5 phosphorylation in platelets. Measuring STAT3 phosphorylation in CD3+ T-cells.
In Vivo
In vivo

BMS-986165 has been identified as a highly potent and selective allosteric TYK2 inhibitor having excellent PK properties across species with minimal profiling liabilities and is orally efficacious with dose-dependent activity in a murine disease model of psoriasis. Significant activity has also been observed with 11 in other murine autoimmune disease models of colitis and lupus.[1]
Animal Research Animal Models 6−8-week-old C57BL/6 female mice
Dosages 7.5 mg/kg, 15 mg/kg, and 30 mg/kg
Administration Oral gavage
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT04671953 Completed Healthy Participants Bristol-Myers Squibb December 18 2020 Phase 1
NCT04209699 Completed Healthy Participants Bristol-Myers Squibb December 27 2019 Phase 1
NCT04113668 Completed Healthy Participants Bristol-Myers Squibb October 1 2019 Phase 1

Chemical lnformation & Solubility

Molecular Weight 425.46 Formula

C20H19D3N8O3
CAS No. 1609392-27-9 SDF --
Smiles CNC(=O)C1=NN=C(C=C1NC2=CC=CC(=C2OC)C3=NN(C=N3)C)NC(=O)C4CC4
Storage (From the date of receipt) 3 years -20°C powder

In vitro
Batch:

DMSO : 85 mg/mL ( (199.78 mM)； Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : Insoluble

Ethanol : Insoluble


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In vivo
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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

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