A2AR-antagonist-1

A2AR-antagonist-1 (compound 38) is an orally active adenosine A2A receptor (A2AR) antagonist (IC50=29 nM) . A2AR-antagonist-1 exhibits anti-tumor activity and mouse liver microsomal metabolic stability (t1/2=86.1 min) . A2AR-antagonist-1 is also a T cells activator, via inhibiting immunosuppressive molecules (LAG-3 and TIM-3) and enhancing effector molecules (GZMB, IFNG, and IL-2) [1].

Product Specifications

CAS Number

[2922920-71-4]

UNSPSC

12352005

Target

Adenosine Receptor

Type

Reference compound

Related Pathways

GPCR/G Protein

Applications

Cancer-programmed cell death

Field of Research

Cancer

Assay Protocol

https://www.medchemexpress.com/a2ar-antagonist-1.html

Solubility

10 mM in DMSO

Smiles

O=C(N(CC1=CC=CC(C(O)(C)C)=C1)C=C2)C=C2C3=NC(N)=NC(C4=C(C)C(C#N)=CC=C4)=C3

Molecular Formula

C27H25N5O2

Molecular Weight

451.52

References & Citations

[1]Zhu C, et al. Discovery of Pyridinone Derivatives as Potent, Selective, and Orally Bioavailable Adenosine A2A Receptor Antagonists for Cancer Immunotherapy. J Med Chem. 2023 Mar 23.