Information diABZI STING agonist (Compound 3) diABZI STING agonist (diABZI STING agonist-1, Compound 3) is a potent non-nucleotide STING agonist and has tremendous potential to improve treatment of cancer in humans. Targets STING In vitro In human PBMCs, compound 3 induces dose-dependent activation of STING and secretion of IFNβ with an EC50 app of 130 nM. In vivo Compound 3 activates secretion of IFNβ, IL-6, TNF, and KC/GROα (also known as CXCL1) in wild-type but not Sting −/− mice. In BALB/c mice administrated 3 mg/kg compound 3 via intravenous injection, compound 3 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). In mice bearing subcutaneous CT-26 tumours, treatment with compound 3 results in significant tumour growth inhibition as measured by tumour volume AUC analysis (P
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diABZI STING agonist (Compound 3)
CAS number:2138498-18-5 molecular formula:C42H51N13O7
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| Chinese alias | - | ||
| English alias | compound 3 [PMID: 30405246] | diABZI | diABZI STING agonist-1 | diABZI STING agonist-1 Tautomerism | HY-112921 | 1-[(2E)-4-[5-carbamoyl-2-(1-ethyl-3-methyl-1H-pyrazole-5-amido)-7-[3-(morpholin-4-yl)propoxy]-1H-1,3-benzodiazol-1-yl]but-2-en-1-yl]-2-(1-ethy | ||
| CAS number | 2138498-18-5 | molecular formula | C42H51N13O7 |
| molecular weight | 849.95 g/mol | Exact mass | - |
| PSA | 247.000 Ų | logp | 1.900 |
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