STING agonist-3, extracted from patent WO2017175147A1 (example 10), is a selective and non-nucleotide small-molecule STING agonist with a pEC 50 and pIC 50 of 7.5 and 9.5, respectively. STING agonist-3 has durable anti-tumor effect and tremendous potential to improve treatment of cancer.
In Vitro
STING agonist-3 exhibits a pEC 50 value of 7.5 in activation of STING in cells, this assay is determined using a luciferase reporter assay in human embryonic kidney cells (HEK293T) co-transfected with plasmids expressing STING and the enzyme firefly luciferase driven by the interferon stimulated response element promoter. ?\nSTING agonist-3 exhibits a pIC 50 value of 9.5 in FRET assay. This is a competition binding assay which aims to determine the binding potency of molecules to the C-terminal Domain (CTD) of human STING. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
