A2AR modulator-1

• Description :

  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].

• 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.

• Shipping Conditions :

  Room temperature

• Scientific Category :

  Reference compound1

• Clinical Information :

  No Development Reported

• Isoform :

  Adenosine A2A receptor (A2AR)