MRS1220 is a highly potent and selective A3 adenosine receptor (A3AR) antagonist with Ki of 0.59 nM for hA3AR. MRS1220 reverses the effect of A3 agonist-elicited inhibition of tumor necrosis factor-α formation in the human macrophage U-937 cell line with IC50 of 0.3 uM. MRS1220 dcreases VEGF secretion in U87MG glioblastoma stem-like cells (GSCs). MRS1220 reduces tumor size and blood vessel formation in vivo.
