E7766 disodium 是一种大环桥连 STING 激动剂，Kd 为 40 nM。E7766 disodium 显示出强大的泛基因型和抗肿瘤活性。
E7766 disodium is a macrocycle-bridged STING agonist with a Kd of 40 nM. E7766 disodium shows potent pan-genotypic and antitumor activities[1].
E7766 disodium 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 disodium in the subcutaneous tumor. E7766 disodium is shown to have potent antitumor activity with long lasting immune memory response in a mouse liver metastatic tumor model[1].
[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.
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