Deucravacitinib (BMS-986165)

For research use only.

Catalog No.S8879

Deucravacitinib (BMS-986165) Chemical Structure

CAS No. 1609392-27-9

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.

Purity & Quality Control

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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

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]

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]

Protocol

Cell Research:

[1]

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  • 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.


    (Only for Reference)
Animal Research:

[1]

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  • 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
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 29 mg/mL (68.16 mM)
Water Insoluble
Ethanol Insoluble

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 425.46
Formula

C20H19D3N8O3

CAS No. 1609392-27-9
Storage powder
in solvent
Synonyms N/A
Smiles CNC(=O)C1=NN=C(C=C1NC2=CC=CC(=C2OC)C3=NN(C=N3)C)NC(=O)C4CC4

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Clinical Trial Information

NCT Number Recruitment interventions Conditions Sponsor/Collaborators Start Date Phases
NCT04772079 Recruiting Drug: BMS-986165|Other: Placebo matching BMS-986165 Plaque Psoriasis Bristol-Myers Squibb March 23 2021 Phase 3
NCT04671953 Recruiting Drug: BMS-986165|Drug: Metformin Healthy Participants Bristol-Myers Squibb December 18 2020 Phase 1
NCT04209699 Completed Drug: BMS-986165|Drug: Famotidine Healthy Participants Bristol-Myers Squibb December 27 2019 Phase 1

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.

Handling Instructions

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JAK Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID