| Description | SR-717 is a cGAMP analog, a non-nucleoside STING agonist that induces a "closed" activation conformation of STING. SR-717 has antitumor activity and promotes activation of immune cells and cross-presentation of antigens. |
| In vitro | 方法：巨噬细胞 THP1 用 SR-717 (3.6 µM) 处理 10 min-6 h，使用 Western Blot 方法检测靶点蛋白表达水平。结果：SR-717 激活 p-STING，及其下游 p-TBK1、p-IRF3、p-p65、p-STAT1 和 p-STAT3。[1]方法：原代人外周血单个核细胞 PBMCs 用 SR-717 (10 µM) 处理 2-6 h，使用 RT-qPCR 方法检测基因表达水平。结果：SR-717 刺激 IFNB1、CXCL10 和 IL6 的激活。[1] |
| In vivo | 方法：为检测体内抗肿瘤活性，将 SR-717 (30 mg/kg) 腹腔注射给携带小鼠皮肤黑色素肿瘤 B16.F10 的 WT 或 Stinggt/gt C57BL/6 小鼠，每天一次，持续七天。结果：SR-717 抑制肿瘤生长以及延长荷癌小鼠的存活时间。SR-717 的抗肿瘤效果表现出对 STING 表达的强制依赖性，在 Stinggt/gt 小鼠中观察到活性缺乏。[1]方法：为检测体内抗肿瘤活性，将 SR-717 (10 mg/kg) 静脉注射给携带小鼠皮肤黑色素肿瘤 B16.F10 的 C57BL/6 小鼠，每两天一次，给药三次。结果：SR-717 在体内具有抗肿瘤活性，可以延长生存期。[2] |
| molecular weight | 351.19 |
| Molecular formula | C15H8F2LiN5O3 |
| CAS | 2375421-09-1 |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year |
| Solubility | DMSO: 25 mg/mL (71.19 mM), Sonication is recommended. |
| References | 1. Chin EN, et al. Antitumor activity of a systemic STING-activating non-nucleotide cGAMP mimetic. Science. 2020 Aug 21;369(6506):993-999. 2. Li L, et al. Cholesterol removal improves performance of a model biomimetic system to co-deliver a photothermal agent and a STING agonist for cancer immunotherapy. Nat Commun. 2023 Aug 22;14(1):5111. |