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

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

Activation of diABZI STING agonist-1 trihydrochloride elicits a type-I interferon response that propagates interferon receptor signalling in tumour-resident dendritic cells and leads to antitumour CD8+ T cell responses in vivo.

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.

2138299-34-8

C42H54Cl3N13O7

959.33

DMSO:125 mg/mL (130.30 mM)
Powder: -20°C for 3 years
In solvent: -80°C for 2 years