Suramin
(Synonyms: 苏拉明) 目录号 : GC37705
A polysulfonated naphthylurea with antiviral, antiparasitic, and anticancer activities
Cas No.:145-63-1
Sample solution is provided at 25 µL, 10mM.
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Suramin is a polysulfonated naphthylurea with antiviral, antiparasitic, and anticancer activities.1 It is negatively charged at physiological pH and therefore binds to various intracellular targets including, but not limited to, ryanodine receptor 1 (IC50 = 4.9 ?M), G protein-coupled receptors, P2 purinergic receptors, PDGF, PKC, transferrin, DNA and RNA polymerases, sirtuins, and various cytokines.1,2,3 It reduces Zika virus infectivity in Vero cells (IC50 = ~2.5-5 ?g/ml).4 In vivo, suramin induces cell cycle arrest at the G2/M phase and apoptosis in L. donovani promastigotes in vitro and reduces hepatic parasitic burden in a mouse model of L. donovani-induced visceral leishmaniasis.5 Suramin (60 mg/kg) reduces tumor volume in patient-derived xenograft (PDX) mouse models of malignant mesothelioma.6 Formulations containing suramin have been used in the treatment of African sleeping sickness.
1.Wiedemar, N., Hauser, D.A., and M?ser, P.100 years of suraminAntimicrob. Agents Chemother.64(3)e01168-01119(2020) 2.Klinger, M., Bofill-Cardona, E., Mayer, B., et al.Suramin and the suramin analogue NF307 discriminate among calmodulin-binding sitesBiochem. J.355(3)827-833(2001) 3.Charlton, S.J., Brown, C.A., Weisman, G.A., et al.PPADS and suramin as antagonists at cloned P2Y- and P2U- purinoceptorsBr. J. Pharmacol.118(3)704-710(1996) 4.Tan, C.W., Sam, I.-C., Chong, W.L., et al.Polysulfonate suramin inhibits Zika virus infectionAntiviral Res.143186-194(2017) 5.Khanra, S., Juin, S.K., Jawed, J.J., et al.In vivo experiments demonstrate the potent antileishmanial efficacy of repurposed suramin in visceral leishmaniasisPLoS Negl. Trop. Dis.14(8)e0008575(2020) 6.Chahinian, A.P., Mandeli, J.P., Gluck, H., et al.Effectiveness of cisplatin, paclitaxel, and suramin against human malignant mesothelioma xenografts in athymic nude miceJ. Surg. Oncol.67(2)104-111(1998)
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Kinase experiment: |
The ATPase assay is performed in a 10 μL reaction mixture containing 20 mM Tris-HCl (pH 7.5), 1 mM DTT, 8 mM MgCl2, 5 μM M13 circular ssDNA, 2.5 μM RecA from the specified bacterial species and increasing concentrations of suramin. The reaction is initiated by the addition of 2 mM [α-32P]ATP, incubated for 30 min at 37°C and stopped by the addition of 25 mM EDTA[2]. |
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Animal experiment: |
Rats: To assess the potential preventive and curative effects of suramin, rats are randomly divided into four groups after MCT injection. In the preventive strategy, the treatment is started on the first day, and one group receives 10 mg/kg suramin intravenously twice weekly for 3 weeks, while a second group receives only the vehicle at the same time points. To assess the potential curative effects of suramin, rats are given MCT and are left untreated for 21 days before being randomly divided into two groups that are subsequently treated with either suramin or vehicle from day 21 to day 42 inclusive. The effect of suramin on survival is evaluated from the day 21 of MCT injection to day 42 corresponding to the treatment period[4]. |
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References: [1]. Jindal HK, et al. Suramin affects DNA synthesis in HeLa cells by inhibition of DNA polymerases. Cancer Res. 1990 Dec 15;50(24):7754-7. |
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| Cas No. | 145-63-1 | SDF | |
| 别名 | 苏拉明 | ||
| Canonical SMILES | O=C(NC1=CC(C(NC2=CC(C(NC3=CC=C(S(=O)(O)=O)C4=CC(S(=O)(O)=O)=CC(S(=O)(O)=O)=C34)=O)=CC=C2C)=O)=CC=C1)NC5=CC(C(NC6=CC(C(NC7=CC=C(S(=O)(O)=O)C8=CC(S(=O)(O)=O)=CC(S(=O)(O)=O)=C78)=O)=CC=C6C)=O)=CC=C5 | ||
| 分子式 | C51H40N6O23S6 | 分子量 | 1297.28 |
| 溶解度 | Soluble in DMSO | 储存条件 | Store at -20°C,protect from light |
| 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 | 0.7708 mL | 3.8542 mL | 7.7084 mL |
| 5 mM | 0.1542 mL | 0.7708 mL | 1.5417 mL |
| 10 mM | 0.0771 mL | 0.3854 mL | 0.7708 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: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet