M1069 (free base) is a selective and orall active, dual A2A/A2B adenosine receptor antagonist with a selectivity of >100 fold against the A1 and A3 receptors. M1069 (free base) counteracts immune-suppressive mechanisms of adenosine, and exhibits anti-tumor activity.
References:
[1]. Rinat Zaynagetdinov, et al. Abstract 3499: M1069 as dual A2A/A2B adenosine receptor antagonist counteracts immune-suppressive mechanisms of adenosine and reduces tumor growth in vivo. Cancer Res (2022) 82 (12_Supplement):3499. [2]. Lillian L Siu, et al. Abstract CT240: A first-in-human study of the dual A2A/A2B adenosine receptor antagonist M1069 in patients with advanced solid tumors. Cancer Res (2022) 82 (12_Supplement):CT240. [3]. Tanzer Eva-Maria, et al. Preparation of thiazolopyridine derivatives as adenosine receptor antagonists: World Intellectual Property Organization, WO2020152132[P]. 2020-07-30.