Etrumadenant (AB928)

Catalog No.S9608 Synonyms: A2aR/A2bR antagonist-1

For research use only.

Etrumadenant (AB928, A2aR/A2bR antagonist-1) is a novel dual A2aR/A2bR antagonist with Kd of 1.4 nM and 2 nM for A2aR and A2bR, respectively.

Etrumadenant (AB928) Chemical Structure

CAS No. 2239273-34-6

Purity & Quality Control

Choose Selective Adenosine Receptor Inhibitors

Biological Activity

Description Etrumadenant (AB928, A2aR/A2bR antagonist-1) is a novel dual A2aR/A2bR antagonist with Kd of 1.4 nM and 2 nM for A2aR and A2bR, respectively.
Targets
A2AR [1]
(Cell-free assay)
A2bR [1]
(Cell-free assay)
1.4 nM(Kd) 2 nM(Kd)
In vitro

Consistent with the ability of adenosine to suppress immune function, AB928 inhibits the ability of adenosine to suppress CD4 or CD8 T cell activation.[2]

In vivo

Established AT-3-OVA tumors treated with AB928 alone has a small but significant decrease in their growth rate. Concurrent treatment with AB928 and chemotherapy results in significantly reduced tumor growth rates, when compared to chemotherapy alone.[2]

Protocol (from reference)

Cell Research:

[2]

  • Cell lines: CD4+ T cells, CD8+ T cells
  • Concentrations: 1 nM, 3 nM, 10 nM, 30 nM
  • Incubation Time: --
  • Method:

    CD4+ or CD8+ T cells are isolated from PBMC using RosetteSep separation and are stimulated with CD2/CD3/CD28 microbeads +/- adenosine/EHNA +/- AB928. Human CD14+ cells are differentiated into moDC for 6 days in IL-4/GM-CSF +/- adenosine/EHNA, +/- AB928. Adenosine is present during moDC activation via IFN-y or LPS. Cells are washed in excess buffer, to remove residual adenosine, prior to setting up the mixed leukocyte reaction (MLR). Supernatants are collected 4 days after initiation of the moDC/CD4 co-culture.

Animal Research:

[2]

  • Animal Models: female C57BL/6 mice
  • Dosages: 100 mg/kg
  • Administration: Oral gavage

Solubility (25°C)

In vitro

Chemical Information

Molecular Weight 426.47
Formula

C23H22N8O

 

CAS No. 2239273-34-6
Storage 3 years -20°C powder
2 years -80°C in solvent
Smiles CC1=C(C=CC=C1C2=CC(=NC(=N2)N)C3=CN(N=N3)CC4=NC(=CC=C4)C(C)(C)O)C#N

In vivo Formulation Calculator (Clear solution)

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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.

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Molarity Calculator

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Clinical Trial Information

NCT Number Recruitment Interventions Conditions Sponsor/Collaborators Start Date Phases
NCT03720678 Completed Drug: etrumadenant|Drug: mFOLFOX GastroEsophageal Cancer|Colorectal Cancer Arcus Biosciences Inc. November 18 2018 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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