ADU-S100

ADU-S100 is a cyclic dinucleotide STING agonist.¹ It induces IFN-β-dependent reporter activity in HEK293T cells expressing human STING, the human STING variants STING HAQ, STING REF, STING AQ, STING Q, or mouse STING when used at a concentration of 10 µM. Intratumoral administration of ADU-S100 (50 µg/tumor per day for three days) reduces tumor growth in wild-type, but not in Sting1^-/-, mice in a B16/F10 murine melanoma model. It decreases primary and secondary tumor volume in a 4T1 murine breast cancer model of tumor rechallenge when intratumorally administered. Unilateral intratumoral administration of ADU-S100 reduces tumor volumes in a bilateral CT26 murine colorectal cancer model. It increases tumor infiltration of natural killer (NK) cells, CD4⁺ T cells, and CD8⁺ T cells, as well as increases immune cell-induced tumor necrosis, in a GL261 murine glioma model when intratumorally administered at a dose of 50 µg/tumor.²

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1. Corrales, L., Glickman, L.H., McWhirter, S.M., et al. Direct activation of STING in the tumor microenvironment leads to potent and systemic tumor regression and immunity. Cell Rep. 11(7), 1018-1030 (2015).

2. Berger, G., Knelson, E.H., Jimenez-Macias, J.L., et al. STING activation promotes robust immune response and NK cell-mediated tumor regression in glioblastoma models. Proc. Natl. Acad. Sci. U.S.A. 119(28), e2111003119 (2022).