A2AR-antagonist-1 (compound 38) is an orally active adenosine A2A receptor (A2AR) antagonist ( IC 50 =29 nM). A2AR-antagonist-1 exhibits anti-tumor activity and mouse liver microsomal metabolic stability (t 1/2 =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 ).
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