STING agonist-3 (Synonyms: CS-0029879, Diamidobenzimidazole STING Agonist, diABZI-3, EX-A3217, HY-103665, STING Agonist-3) |
| Katalog-Nr.GC37692 |
STING-Agonist-3, extrahiert aus dem Patent WO2017175147A1 (Beispiel 10), ist ein selektiver und nicht-Nukleotid-STING-Agonist aus kleinen MolekÜlen mit einem pEC50 und pIC50 von 7,5 bzw. 9,5. Der STING-Agonist-3 hat eine dauerhafte Antitumorwirkung und ein enormes Potenzial zur Verbesserung der Krebsbehandlung.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 2138299-29-1
Sample solution is provided at 25 µL, 10mM.
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STING agonist-3 is a selective small-molecule STING agonist. STING agonist-3 is a non-nucleotide STING agonist which has durable anti-tumor effect and tremendous potential to improve treatment of cancer[1].
STING agonist-3 (Compound 3) induces dose-dependent activation of STING and secretion of IFN-β with ECapp50s of 130 nM,186 nM in human PBMCs and Mouse PBMCs[1].
STING agonist-3 (Compound 3) (subcutaneous injection; 2.5mg/kg) activates secretion of IFN-β, IL-6, TNF-α, and KC/GROα (CXCL1) in wild-type but not Sting-/- mice, induces STING-dependent activation of type-I interferon and pro-inflammatory cytokines in vivo[1].STING agonist-3 (Compound 3) (subcutaneous injection; 3 mg/kg) exhibits systemic exposure with a half-life of 1.4 h and achieves systemic concentrations with EC50=200 ng /ml for mouse STING[1].STING agonist-3 (Compound 3) (injection intravenously; 1.5 mg/kg) results in significant tumor growth inhibition, and improves survival with 8 out of 10 mice remaining tumors free at day 43[1]. Animal Model: Mice with approximately 100 mm3 subcutaneous CT-26 tumors[1]
[1]. Ramanjulu JM et al. Design of amidobenzimidazole STING receptor agonists with systemic activity. Nature. 2018 Dec;564(7736):439-443.
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