diABZI STING agonist-1 (tautomerism)

diABZI STING agonist-1 tautomerism is a tautomerism of diABZI STING agonist-1 (HY-112921A). diABZI STING agonist-1 tautomerism is a selective stimulator of interferon genes (STING) receptor agonist, with EC₅₀s of 130, 186 nM for human and mouse, respectively^[1]. IC50 & Target:EC50: 130 nM (human STNG in PBMCs) ^[1]. In Vitro:diABZI STING agonist-1 tautomerism is a selective stimulator of interferon genes (STING) receptor agonist, with EC₅₀s of 130, 186 nM for human and mouse, respectively. At a concentration of 1 μM, diABZI STING agonist-1 (compound 3) demonstrates high selectivity against more than 350 kinases tested^[1]. In Vivo:diABZI STING agonist-1 (subcutaneous injection; 2.5 mg/kg) tautomerism induces STING-dependent activation of type-I interferon and pro-inflammatory cytokines in vivo^[1].
diABZI STING agonist-1 (intravenous injection; 3 mg/kg) tautomerism exhibits systemic exposure with a half-life of 1.4 h and achieves systemic concentrations greater than the half-maximal effective concentration (EC₅₀) for mouse STING (200 ng/mL)^[1].
diABZI STING agonist-1 (intravenous injection; 1.5 mg/kg; 43 days) tautomerism results in significant tumour growth inhibition and significantly improves survival with 8 out of 10 mice remaining tumor free at the end of the study on day 43^[1].