diABZI STING agonist (Compound 3) - 98%, high purity , CAS No.2138498-18-5, Agonist of stimulator of interferon response cGAMP interactor 1

Item Number

D414188

• Synonyms: 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
• Specifications & Purity: Moligand™, ≥98%
• Biochemical and Physiological Mechanisms: 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.
• Storage Temp: Store at -20°C
• Shipped In: Ice chest + Ice pads
• Grade: Moligand™
• Action Type: AGONIST
• Mechanism of action: Agonist of stimulator of interferon response cGAMP interactor 1

Product Description

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<0.001), and significantly improves survival (P<0.001) with 8 out of 10 mice remaining tumour free at the end of the study on day 43.