Deucravacitinib (BMS-986165)

Catalog No.S8879

For research use only.

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

CAS No. 1609392-27-9

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 (from reference)

Cell Research:

[1]

  • 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.

Animal Research:

[1]

  • 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

Solubility (25°C)

In vitro

Chemical Information

Molecular Weight 425.46
Formula

C20H19D3N8O3

CAS No. 1609392-27-9
Storage 3 years -20°C powder
2 years -80°C in solvent
Smiles CNC(=O)C1=NN=C(C=C1NC2=CC=CC(=C2OC)C3=NN(C=N3)C)NC(=O)C4CC4

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Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
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Molarity Calculator

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Clinical Trial Information

NCT Number Recruitment Interventions Conditions Sponsor/Collaborators Start Date Phases
NCT04671953 Completed 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
NCT04113668 Completed Drug: BMS-986165|Drug: diflunisal Healthy Participants Bristol-Myers Squibb October 1 2019 Phase 1

(data from https://clinicaltrials.gov, updated on 2022-08-01)

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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