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STING agonist-3
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
STING agonist-3图片
CAS NO:2138299-29-1
包装与价格:
包装价格(元)
10mM (in 1mL DMSO)电议
5mg电议
10mg电议
25mg电议

产品介绍
STING agonist-3 是一种选择性小分子STING 激动剂。STING agonist-3 是非核苷酸 STING 激动剂,具有持久的抗肿瘤和改善癌症治疗的巨大潜力。
Cas No.2138299-29-1
Canonical SMILESO=C(N)C1=CC=C(N(C(NC(C2=CC(C)=NN2CC)=O)=N3)C/C=C/CN4C5=C(N=C4NC(C6=CC(C)=NN6CC)=O)C=C(C(N)=O)C=C5OCCCO)C3=C1
分子式C37H42N12O6
分子量750.81
溶解度DMSO: 125 mg/mL (166.49 mM)
储存条件Store at -20°C
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping ConditionEvaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
产品描述

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.