Biological Activity
E7766 diammonium salt is a macrocycle-bridged STING agonist with a Kd of 40 nM. E7766 diammonium salt shows potent pan-genotypic and antitumor activities[1].
E7766 diammonium salt inhibits four human STING variants, human wild-type, HAQ, AQ and REF STING proteins, with EC50 values of 1 μM, 2.2 μM, 1.2 μM and 4.9 μM, respectively[1].
In murine colon cancer model, a single intratumoral injection of 10 mg/kg E7766 diammonium salt in the subcutaneous tumor. E7766 diammonium salt is shown to have potent antitumor activity with long lasting immune memory response in a mouse liver metastatic tumor model[1].
References
[1]. Dae-Shik Kim, et al. E7766, a Macrocycle-Bridged Stimulator of Interferon Genes (STING) Agonist with Potent Pan-Genotypic Activity. ChemMedChem. 2021 Jun 7;16(11):1740-1743.
