Etrumadenant (AB928)

Catalog No.S9608 Batch:S960801

Technical Data

Formula

C₂₃H₂₂N₈O

Molecular Weight

426.47

CAS No.

2239273-34-6

Solubility (25°C)*

In vitro

DMSO

85 mg/mL (199.31 mM)

Ethanol

5 mg/mL (11.72 mM)

Water

Insoluble

In vivo (Add solvents to the product individually and in order)

Clear solution	5% DMSO 1 95% Corn oil	0.7mg/ml	Taking the 1 mL working solution as an example, add 50 μL of 14 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results.
Clear solution	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O	4.25mg/ml	Taking the 1 mL working solution as an example, add 50 μL of 85 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.

* <1 mg/ml means slightly soluble or 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.
* Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

Preparing Stock Solutions

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 Assay:^{^[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 Study:^{^[2]}	Animal Models female C57BL/6 mice Dosages 100 mg/kg Administration Oral gavage

Cell Assay:^{^[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 Study:^{^[2]}

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

References

Selleck's Etrumadenant (AB928) has been cited by 1 publication

Cordyceps militarisExtract and the Main Component, Cordycepin, Modulate the Functions of Prostate Cancer Cells Partially Through the Adenosine A1 [ Natural Product Communications, 2022, 2022;17(10)]	PubMed: none

Cordyceps militarisExtract and the Main Component, Cordycepin, Modulate the Functions of Prostate Cancer Cells Partially Through the Adenosine A1 [ Natural Product Communications, 2022, 2022;17(10)]

PubMed: none

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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

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