A2AR modulator-1

A2AR modulator-1 (Compound 45) is a selective negative allosteric adenosine A2a receptor (A2aR) modulator with an IC50 value of 9 nM. A2AR modulator-1 reduces the affinity of endogenous adenosine for the receptor and inhibits cAMP signaling pathway activation. A2AR modulator-1 potently restores pCREB phosphorylation in CD4+ T cells, reversing immunosuppression in the tumor microenvironment, and shows potential to suppress tumor growth and metastasis in triple-negative breast cancer models[1].

Product Specifications

CAS Number

[3007566-23-3]

UNSPSC

12352005

Target

Adenosine Receptor

Related Pathways

GPCR/G Protein

Applications

Cancer-Kinase/protease

Field of Research

Cancer

Smiles

N#CC1=C(C2=CC=CC(C3=CC=CN=C3)=C2)C(C#N)=C(N4CCCCC4)N=C1N

Molecular Formula

C23H20N6

Molecular Weight

380.45

References & Citations

[1]Boujut M, et al. Discovery of the First Efficacious Adenosine 2A Receptor Negative Allosteric Modulators for High Adenosine Cancer Immunotherapies. J Med Chem. 2025 Feb 27;68 (4) :4059-4078.