diABZI STING agonist-1 (trihydrochloride) is stimulator of interferon genes (STING) receptor agonist.

diABZI STING agonist-1 trihydrochloride 是选择性的干扰素基因刺激受体(STING)激动剂，在人和小鼠中都能发挥作用，其 EC50值分别为 130 和 186 nM。

方法：diABZI STING agonist-1 (trihydrochloride) （3mg/kg，静脉注射 ）在BALB/c小鼠体内，观察小鼠体内的药代动力学谱。
结果：diABZI STING agonist-1 (trihydrochloride) 全身性暴露，半衰期为1.4 h，全身性浓度大于小鼠STING的半最大有效浓度(EC50) (200 ng /ml)。[1]
方法：diABZI STING agonist-1 (trihydrochloride) （1.5 mg/kg, 1、4和8天,静脉注射）在皮下CT-26肿瘤的小鼠中,通过肿瘤体积AUC分析。
结果：diABZI STING agonist-1 (trihydrochloride) 对肿瘤生长有明显的抑制作用，显著提高了生存率(P<0.001)。[1]

To evaluate the potential therapeutic effects of systemically administered diABZI STING agonist-1 trihydrochloride, tested the efficacy of intravenously delivered diABZI STING in a syngeneic mouse model of colorectal tumours (CT-26) in BALB/c mice.?We first established the pharmacokinetic profile of STING in BALB/c mice following intravenous injection of 3 mg/kg .?STING exhibited systemic exposure with a half-life of 1.4 h and achieved systemic concentrations greater than the half-maximal effective concentration (EC50) for mouse STING (~200 ng/ml).?Next, we tested an intermittent dosing paradigm in which 1.5 mg/kg STING was injected intravenously on days 1, 4, and 8 in mice with approximately 100 mm^3 subcutaneous CT-26 tumours.?Treatment with STING resulted in significant tumour growth inhibition as measured by tumour volume AUC analysis (P<0.001), and significantly improved survival (P<0.001) with 8 out of 10 mice remaining tumour free at the end of the study on day 43.