TAK-676 (Dazostinag disodium) is a potent, selective stimulator of interferon genes (STING) agonist with highly selective binding and activation of STING proteins from various species, with Kd values of 0.01 uM, 0.008 uM, 0.011 uM, and 0.027 uM for mouse, rat, cynomolgus monkey, and human STING orthologs, respectively.
TAK-676 (Dazostinag disodium) shows EC50 of 0.3 uM in vitro by using reporter assays using HEK293T cells transiently transfected with human WT STING (R232).
TAK-676 (Dazostinag disodium) has IFN activation EC50 of 1.53 uM THP1 Dual and RAW-Lucia ISG reporter cell lines.
TAK-676 dose-dependently induce STING-TBK1-IRF3 activation.
TAK-676 promotes the activation of dendritic cells, natural killer cells, and T cells in preclinical models.
TAK-676 induces dose-dependent cytokine responses and increases the activation and proliferation of immune cells within the TME and tumor-associated lymphoid tissue.