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：2138299-29-1
分子式：C37H42N12O6
分子量：750.81
纯度：98%
存储：Store at -20°C

Background:

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.