Home GPCR & G Protein Adenosine Receptor antagonist Etrumadenant (AB928) For research use only.

Etrumadenant (AB928)

Synonyms: A2aR/A2bR antagonist-1

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

Etrumadenant (AB928) Chemical Structure

CAS No. 2239273-34-6

Purity & Quality Control

Batch: S960801 DMSO]85 mg/mL]false]Ethanol]5 mg/mL]false]Water]Insoluble]false Purity: 99.8%
99.8

Etrumadenant (AB928) Related Products

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
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]
Cell Research 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.
In Vivo
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]
Animal Research Animal Models female C57BL/6 mice
Dosages 100 mg/kg
Administration Oral gavage
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT03720678 Completed
GastroEsophageal Cancer|Colorectal Cancer
Arcus Biosciences Inc.
 November 18 2018 Phase 1

Chemical Information & Solubility

Molecular Weight 426.47 Formula

C23H22N8O

 
CAS No. 2239273-34-6 SDF --
Smiles CC1=C(C=CC=C1C2=CC(=NC(=N2)N)C3=CN(N=N3)CC4=NC(=CC=C4)C(C)(C)O)C#N
Storage (From the date of receipt) 3 years -20°C powder

In vitro
Batch:

DMSO : 85 mg/mL ( (199.31 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 5 mg/mL

Water : Insoluble


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In vivo
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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

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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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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