SHR170008 is a highly potent, small molecule CD73 inhibitor with IC50 of 0.05 nM against human CD73 soluble enzyme.
SHR170008 inhibits endogenous membrane-bound CD73 using CD73-expressing human melanoma cell line A375 with IC50 of 0.051 nM, much stronger than AMPCP (CI50=16 nM).
SHR170008 reverses the inhibitory effect of adenosine from AMP in the activation and proliferation of CD8+ T cells as well as Granzyme B+ cells in CD8+ cells.
SHR170008 significantly reverses the suppression of IFNγ production with average EC50=110 ± 51 nM in human PBMC.
SHR170008 exhibited in vivo anti-tumor efficacy and synergistic effects in combination with anti-PD-1 mAb in EMT6 mouse syngeneic breast tumor model.
