AB-680

AB-680 is an inhibitor of ecto-5'-nucleotidase, also known as CD73 (IC₅₀ = 0.043 nM in CHO cells expressing the human enzyme).¹ It is selective for ecto-5'-nucleotidase over nucleoside triphosphate diphosphorylase 1 (NTPDase 1), NTPDase 2, NTPDase 3, and NTPDase 8 (IC₅₀s = >10 µM for all). AB-680 also inhibits ecto-5'-nucleotidase activity in isolated human and mouse CD8⁺ T cells and isolated human peripheral blood mononuclear cells (PBMCs; IC₅₀s = 0.008, 0.66, and 0.011 nM, respectively). It reverses AMP-induced decreases in the proliferation of, and IFN-γ and granzyme B secretion by, isolated human CD4⁺ and CD8⁺ T cells when used at a concentration of 200 nM.² AB-680 (10 mg/kg) reduces tumor volume in a B16/F10 murine melanoma model alone and in combination with an antibody targeting programmed cell death protein 1 (PD-1).

WARNING This product is not for human or veterinary use.

1. Lawson, K.V., Kalisiak, J., Lindsey, E.A., et al. Discovery of AB680: A potent and selective inhibitor of CD73. J. Med. Chem. 63(20), 11448-11468 (2020).

2. Piovesan, D., Tan, J.B.L., Becker, A., et al. Targeting CD73 with AB680 (quemliclustat), a novel and potent small-molecule CD73 inhibitor, restores immune functionality and facilitates antitumor immunity. Mol. Cancer Ther. 21(6), 948-959 (2022).