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An adenosine A2 receptor antagonist
AZD4635 is a potent and selective, orally available adenosine A2A receptor (A2AR) antagonist. AZD4635 binds to human A2AR with a Ki of 1.7 nM and with > 30-fold selectivity over other adenosine receptors[1].
In the presence of 0.1, 1 and 10 μM adenosine, the IC50s of AZD4635 for inhibition of cAMP production are 0.79, 10.0 and 142.9 nM, respectively[1].
参考文献:
[1]. Alexandra Borodovsky, et al. Abstract 5580: Preclinical pharmacodynamics and antitumor activity of AZD4635, a novel adenosine 2A receptor inhibitor that reverses adenosine mediated T cell suppression. AACR; Cancer Res 2017;77(13 Suppl):Abstract nr 5580.
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