STING agonist-3 (Synonyms: CS-0029879, Diamidobenzimidazole STING Agonist, diABZI-3, EX-A3217, HY-103665, STING Agonist-3) |
| Catalog No.GC37692 |
특허 WO2017175147A1(실시예 10)에서 추출한 STING 효능제-3은 pEC50 및 pIC50이 각각 7.5 및 9.5인 선택적 및 비-뉴클레오티드 소분자 STING 효능제입니다. STING agonist-3는 지속적인 항종양 효과와 암 치료를 개선할 수 있는 엄청난 잠재력을 가지고 있습니다.
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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