Etrumadenant

Etrumadenant (CAS No.: 2239273-34-6) is a synthetic small-molecule, selective adenosine receptor A2A/A2B dual antagonist, classified as a chemical probe for purinergic signaling pathway research. It is primarily intended for biomedical research and drug discovery settings such as immuno-oncology, and is used to elucidate adenosine-mediated immunosuppression and its regulation of the tumor microenvironment. By blocking the Gs protein-coupled A2A and A2B receptors, it attenuates downstream cAMP-dependent suppression of T cell receptor and antigen-presenting cell function, thereby restoring the activation and effector output of human CD4/CD8 T cells and monocyte-derived dendritic cells in vitro; in receptor binding and cell-based assays, it exhibits low-nanomolar affinity and antagonistic activity toward A2A and A2B, with relatively selective low impact on A1 and A3 receptors, placing its overall in vitro activity in the nanomolar range. In research, it has been used in syngeneic animal models to examine the effects of the adenosine axis on tumor-associated phenotypes, and in combination with chemotherapeutic agents or programmed cell death protein 1 pathway blockade to explore synergistic effects, supporting mechanism-oriented studies, target validation, and combination regimen screening. Typical applications include immune cell function assessment, co-culture systems, and in vitro and in vivo studies centered on the CD39/CD73—adenosine axis; the concentrations or doses used in experiments generally depend on the specific experimental design and research objectives. This product is for research use only.