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

diABZI STING agonist-1 trihydrochloride is a selective stimulator of interferon genes receptor (STING) agonist with EC50 values ​​of 130 and 186 nM in humans and mice.

METHODS: diABZI STING agonist-1 (trihydrochloride) (3mg/kg, intravenous injection) was administered to BALB/c mice to observe the pharmacokinetic spectrum in the mice.
RESULTS diABZI STING agonist-1 (trihydrochloride) was systematically exposed, with a half-life of 1.4 h, and the systemic concentration was greater than the half-maximum effective concentration (EC50) of mouse STING (200 ng/ml). [1]
METHODS: diABZI STING agonist-1 (trihydrochloride) (1.5 mg/kg, 1, 4 and 8 days, intravenous injection) in mice with subcutaneous CT-26 tumors was analyzed by tumor volume AUC.
RESULTS diABZI STING agonist-1 (trihydrochloride) had a significant inhibitory effect on tumor growth and significantly improved survival rate (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.