| Description | diABZI STING agonist-1 (trihydrochloride) is stimulator of interferon genes (STING) receptor agonist. |
| In vitro | 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. |
| Animal experiments | 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. |
| molecular weight | 959.32 |
| Molecular formula | C42H54Cl3N13O7 |
| CAS | 2138299-34-8 |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year |
| Solubility | DMSO: 125 mg/mL (130.30 mM) |
| References | 1. Ramanjulu JM, et al. Design of amidobenzimidazole STING receptor agonists with systemic activity. Nature. 2018 Nov 7. |
| Citations | 1. Cao D, Duan L, Huang B, et al.The SARS-CoV-2 papain-like protease suppresses type I interferon responses by deubiquitinating STING.Science Signaling.2023, 16(783): eadd0082. |