SR-717
目录号 : GC61293
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。
Cas No.:2375421-09-1
Sample solution is provided at 25 µL, 10mM.
;)
,-1-7$$$37316672.jpg');)
;)
;)
$$$36806353.jpg');)
;33(7)%EF%BC%9A546-561$$$37156877.jpg');)
;)
;)
;)
%201124-1138.$$$35908550.jpg');)
%20766-780.$$$37100057.jpg');)
%20418-432.$$$36893736.jpg');)
%EF%BC%9A-240-255.$$$35108512.jpg');)
533-545$$$36543525.jpg');)
%201-13.$$$36600053.jpg');)
;)
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 ].
| 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. |
|
| Cas No. | 2375421-09-1 | SDF | |
| Canonical 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 |
| 溶解度 | DMSO: 14.29 mg/mL (40.69 mM); Water: < 0.1 mg/mL (insoluble) | 储存条件 | 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℃，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。 | ||
| 制备储备液 | |||
 |
1 mg | 5 mg | 10 mg |
| 1 mM | 2.8475 mL | 14.2373 mL | 28.4746 mL |
| 5 mM | 0.5695 mL | 2.8475 mL | 5.6949 mL |
| 10 mM | 0.2847 mL | 1.4237 mL | 2.8475 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
Quality Control & SDS
- View current batch:
- Purity: >99.50%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet