2',3'-cGAMP
(Synonyms: 2'-3'-cyclic GMP-AMP) 目录号 : GC19989
2',3'-cGAMP是一种特异性的STING受体激动剂，其作用机理主要是激活STING信号通路，促进干扰素和炎症因子的产生。
Cas No.:1441190-66-4
Sample solution is provided at 25 µL, 10mM.
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2',3'-cGAMP is a specific agonist of the STING receptor, and its mechanism of action primarily involves activating the STING signaling pathway, promoting the production of interferons and inflammatory cytokines. 2',3'-cGAMP plays an important role in the innate immune pathway of mammals, responsible for the surveillance of cytoplasmic DNA. The Kd value of 2',3'-cGAMP binding to STING is 3.79 nM[1]. 2',3'-cGAMP is commonly used in research on immune regulation, antiviral immunity, and cancer treatment.
In vitro, 2',3'-cGAMP (2.2, 4.4, 8.75, 17, 35 μM) treatment of PC 3 cells for 48 hours has an IC50 value of 11.46 μM[2]. Treating the PC 3 cell line with 2',3'-cGAMP (4 µg/ml) for 10 minutes activates STING[3].
In vivo, 10 μg of 2',3'-cGAMP is as effective as 200 μg of PD-L1 antibody in combating melanoma in C57 BL/6 mice. Titration experiments show that 2',3'-cGAMP enhances the antitumor effect of the PD-L1 antibody in a dose-dependent manner[4].
References:
[1] Zhang X, et al. Cyclic GMP-AMP containing mixed phosphodiester linkages is an endogenous high-affinity ligand for STING. Mol Cell. 2013 Jul 25;51(2):226-35.
[2] Rezaei M .09-P53. Docetaxel Enhances the Expression of STING Protein in PC3 Prostate Cancer Cells, and cGAMP Attenuates This Effect[C]. Benchmarking an Artificial Intelligence Method for Fast Diagnosis of Rare Genetic Disease.2020.
[3] Hannes S , Karlowitz R , Wijk S J L V .The Smac mimetic BV6 cooperates with STING to induce necroptosis in apoptosis-resistant pancreatic carcinoma cells[J].Cell Death & Disease.2024.
[4] Wang, H. et al. cGAS is essential for the antitumor effect of immune checkpoint blockade. Proc. Natl Acad. Sci. USA 114, 1637–1642 (2017).
2',3'-cGAMP是一种特异性的STING受体激动剂，其作用机理主要是激活STING信号通路，促进干扰素和炎症因子的产生。2',3'-cGAMP 在哺乳动物先天免疫途径中起着重要作用，负责胞质DNA的监测。2',3'-cGAMP 结合STING的Kd值为3.79 nM[1]。2',3'-cGAMP通常用于研究免疫调节、抗病毒免疫和肿瘤治疗等领域。
在体外，2',3'-cGAMP(2.2、4.4、8.75、17、35 μM) 处理PC 3细胞48小时，其IC50值为11.46 μM[2]。用2',3'-cGAMP (4 µg/ml) 处理PC 3细胞系10分钟，来激活STING[3]。
在体内，10 μg 2',3'-cGAMP与200 μg PD-L1抗体一样有效具备抗C57 BL/6 小鼠黑色素肿瘤作用。滴定实验表明，2',3'-cGAMP以剂量依赖性方式增强PD-L1抗体的抗肿瘤作用[4]。
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Cell experiment [1]: |
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Cell lines |
PC3 cell |
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Preparation method |
Cell toxicity was measured using the method of MTT. After 24 hours of incubation, cells were exposed to docetaxel for 48 hours at concentrations of 2.2, 4.4, 8.75, 17.5 and 35 μM 2',3'-cGAMP. After 48h incubation, the cell suspension was washed with PBS. |
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Reaction Conditions |
2.2, 4.4, 8.75, 17.5 and 35 μM; 48h |
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Applications |
The 2',3'-cGAMP has cytotoxic effects, IC50 was 11.46 μM. |
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Animal experiment [2]: |
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Animal models |
C57 BL/6 mice |
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Preparation method |
After melanoma cell inoculation, C57 BL/6 mice were treated with 3 μg, 10 μg of 2′3′-cGAMP or 200 μg of PD-L1 antibody on days 4, 8 and 12 respectively (n = 4-5 in each group). A total of 50 μL of 2′3′-cGAMP in PBS at the indicated concentrations was injected into the muscles of the hind legs, and the tumor volume was measured. |
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Dosage form |
3 μg/10 μg；4, 8 and 12days；i.m. |
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Applications |
10 μg of 2',3'-cGAMP was as effective as 200 μg of the PD-L1 antibody, and the combination treatment was even more effective. Titration experiment showed that 2',3'-cGAMP enhanced the antitumor effects of PD-L1 antibody in a dose-dependent manner. |
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References: [1] Rezaei M .09-P53. Docetaxel Enhances the Expression of STING Protein in PC3 Prostate Cancer Cells, and cGAMP Attenuates This Effect[C]. Benchmarking an Artificial Intelligence Method for Fast Diagnosis of Rare Genetic Disease.2020. [2] Wang, H. et al. cGAS is essential for the antitumor effect of immune checkpoint blockade. Proc. Natl Acad. Sci. USA 114, 1637–1642 (2017). |
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| Cas No. | 1441190-66-4 | SDF | |
| 别名 | 2'-3'-cyclic GMP-AMP | ||
| 分子式 | C20H24N10O13P2 | 分子量 | 674.41 |
| 溶解度 | Water : 5 mg/mL (7.41 mM; ultrasonic and warming and heat to 60°C) | 储存条件 | -20°C, sealed storage, away from moisture |
| 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。 |
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| 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 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 1.4828 mL | 7.4139 mL | 14.8278 mL |
| 5 mM | 0.2966 mL | 1.4828 mL | 2.9656 mL |
| 10 mM | 0.1483 mL | 0.7414 mL | 1.4828 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
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- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
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