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diABZI STING agonist (Compound 3)

CAS number:2138498-18-5    molecular formula:C42H51N13O7

overview

compound introduction

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

Specs

Chinese alias-
English aliascompound 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 number2138498-18-5molecular formulaC42H51N13O7
molecular weight849.95 g/molExact mass-
PSA247.000 Ųlogp1.900

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