GlpBio

SR-717

目录号: GC61293纯度: >99.50%
SR-717 是一种稳定的环磷酸鸟苷-磷酸腺苷 (cGAMP) 模拟物，具有抗肿瘤活性。
SR-717
Cas No.: 2375421-09-1
规格价格库存数量操作
1mg¥477.00现货
1
5mg¥1,050.00现货
1
10mg¥1,750.00现货
1
25mg¥3,150.00现货
1
10mM (in 1mL DMSO)¥1,155.00现货
1
电话: 400-920-5774Email: sales@glpbio.cn

文献被引

本产品暂无引用记录;以下为 GlpBio 产品在 Nature / Cell / Science 等顶刊的客户引用样例
  • Nature cover
    Nature
    641, 529–536 (2025)
  • Nature cover
    Nature
    628, 630–638 (2024)
  • Nature cover
    Nature
    632, 686–694 (2024)
  • Nature cover
    Nature
    618, 1017–1023 (2023)
  • Nature cover
    Nature
    610, 366–372 (2022)
  • Cell cover
    Cell
    187(9):2288-2304 (2024)
  • Cell cover
    Cell
    183(7):1867-1883 (2020)
  • Science cover
    Science
    388(6745) (2025)
  • Science cover
    Science
    387(6739) (2025)
  • Science cover
    Science
    387(6734) (2025)
  • Cell Research cover
    Cell Research
    35, 97–116 (2025)
  • Cell Research cover
    Cell Research
    34, 683–706 (2024)
  • Cell Research cover
    Cell Research
    33, 273–287 (2023)
  • Cell Research cover
    Cell Research
    33, 546–561 (2023)
  • Cell Research cover
    Cell Research
    33, 904–922 (2023)
  • Cell Research cover
    Cell Research
    31, 1291–1307 (2021)

产品描述 Description

SR-717 is a stable cyclic guanosine monophosphate-adenosine monophosphate (cGAMP) mimetic, Antitumor activity[1]. The cGAS-STING pathway promotes the senescence of cancer cells, induces apoptosis of cancer cells, and increases the protective effect of cytotoxic T cells and natural killer cell-mediated cytotoxicity[4]. cGAS-STING pathway plays an important role in the chronic inflammatory status in various organs[5].SR-717 as a non-nucleotide STING agonist with EC50s of 2.1 μM and 2.2 μM in ISG-THP1 (WT) and ISG-THP1 cGAS KO (cGAS KO) cell lines, respectively.

Pharmacological targeting of cGAS/STING-YAP signaling by both a small-molecule STING agonist, SR-717 that blocks the profibrotic activity of endothelial YAP, attenuated liver and kidney fibrosis[2].

By STING agonist SR-717, activation of cGAS-STING pathway induced increased apoptosis, inflammation, and oxidative stress via regulating ERS and therefore resulted in pulmonary edema and pathological injury in the lungs of I/R rats[3].

References:
[1]: Chin EN, Yu C, et,al. Antitumor activity of a systemic STING-activating non-nucleotide cGAMP mimetic. Science. 2020 Aug 21;369(6506):993-999. doi: 10.1126/science.abb4255. PMID: 32820126.
[2]: Wang L, Zhang Y, et,al. Pharmacological targeting of cGAS/STING-YAP axis suppresses pathological angiogenesis and ameliorates organ fibrosis. Eur J Pharmacol. 2022 Sep 2;932:175241. doi: 10.1016/j.ejphar.2022.175241. Epub ahead of print. PMID: 36058291.
[3]: Huang R, Shi Q, et,al. Inhibition of the cGAS-STING Pathway Attenuates Lung Ischemia/Reperfusion Injury via Regulating Endoplasmic Reticulum Stress in Alveolar Epithelial Type II Cells of Rats. J Inflamm Res. 2022 Sep 5;15:5103-5119. doi: 10.2147/JIR.S365970. PMID: 36091334; PMCID: PMC9462969.
[4]: Du H, Xu T, et,al. cGAS-STING signaling in cancer immunity and immunotherapy. Biomed Pharmacother. 2021 Jan;133:110972. doi: 10.1016/j.biopha.2020.110972. Epub 2020 Nov 27. PMID: 33254021.
[5]: Bao T, Liu J, et,al. The cGAS-STING pathway: more than fighting against viruses and cancer. Cell Biosci. 2021 Dec 14;11(1):209. doi: 10.1186/s13578-021-00724-z. PMID: 34906241; PMCID: PMC8670263.

SR-717 是一种稳定的环磷酸鸟苷-磷酸腺苷 (cGAMP) 模拟物，具有抗肿瘤活性[1]。 cGAS-STING通路促进癌细胞衰老，诱导癌细胞凋亡，增加细胞毒性T细胞和自然杀伤细胞介导的细胞毒性的保护作用[4]。 cGAS-STING通路在多种器官的慢性炎症状态中起着重要作用[5]。SR-717作为一种非核苷酸STING激动剂，在ISG-THP1中的EC50分别为2.1 μM和2.2 μM（ WT)和ISG-THP1 cGAS KO (cGAS KO)细胞系。

小分子 STING 激动剂 SR-717 对 cGAS/STING-YAP 信号的药理学靶向作用可阻断内皮 YAP 的促纤维化活性，减轻肝肾纤维化[2]。< /p>\n

通过 STING 激动剂 SR-717，cGAS-STING 通路的激活通过调节 ERS 诱导细胞凋亡、炎症和氧化应激增加，从而导致 I/R 大鼠肺部的肺水肿和病理损伤[3 ].

实验参考方法 Experimental Reference Method

Cell experiment [1]:

Cell lines

human umbilical vein endothelial cells (HUVECs)

Preparation Method

The cells were exposed to 2 μM SR-717 and challenged with 10% fetal bovine serum (FBS) for 2 h.

Reaction Conditions

2 μM SR-717 for two hours

Applications

Pharmacological targeting of cGAS/STING-YAP signaling by both a small-molecule STING agonist, SR-717 that blocks the profibrotic activity of endothelial YAP, attenuated liver and kidney fibrosis.
Animal experiment [2]:

Animal models

Stinggt/gt mice

Preparation Method

The tumor growth was detected by intraperitoneal injection of SR-717 (30 mg/kg, once a day, for 1 week).

Dosage form

30 mg/kg SR-717 once-per-day for 1 week

Applications

SR-717 (30 mg/kg intraperitoneally for 7 days) displays antitumor activity; promots the activation of CD8+ T, natural killer, and dendritic cells in relevant tissues; and facilitates antigen cross-priming

References:

[1]. Wang L, Zhang Y, et,al. Pharmacological targeting of cGAS/STING-YAP axis suppresses pathological angiogenesis and ameliorates organ fibrosis. Eur J Pharmacol. 2022 Sep 2;932:175241. doi: 10.1016/j.ejphar.2022.175241. Epub ahead of print. PMID: 36058291.

[2]. Chin EN, Yu C, et,al. Antitumor activity of a systemic STING-activating non-nucleotide cGAMP mimetic. Science. 2020 Aug 21;369(6506):993-999. doi: 10.1126/science.abb4255. PMID: 32820126.

产品文档 Product Documents

Purity:>99.50%

化学性质Chemical Properties

CAS 号
2375421-09-1
SMILES
O=C(O[Li])C1=CC(F)=C(F)C=C1NC(C2=NN=C(N3C=CN=C3)C=C2)=O
分子式
C15H8F2LiN5O3
分子量
351.19 g/mol
溶解性
DMSO: 14.29 mg/mL (40.69 mM); Water: &lt; 0.1 mg/mL (insoluble)
保存条件
Store at -20°C
General tips
请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。
为了提高溶解度，请将管子加热至 37°C，然后在超声波浴中震荡一段时间。
Shipping Condition
评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备 RT，或根据请求配备蓝冰。

计算工具摩尔浓度 / 稀释 / 分子量 / 单位换算 / 体内配方 / 溶解度

g/mol