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.
;)
,-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');)
;)
Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
|
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]. |
|
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]. |
|
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. |
|
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)
| 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。 |
||
| 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 | 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。
Suramin's development: what did we learn?
Invest New Drugs 2002 May;20(2):209-19.PMID:12099581DOI:10.1023/a:1015666024386.
Suramin, a polysulphonated napthylurea, has been extensively evaluated over the past 10 years as an anticancer agent, with the most interest in the treatment of prostate cancer. Early clinical results were promising with response rates of up to 70% being reported. However, a recent double-blind study showed only modest palliative effect in patients with androgen independent prostate cancer. In retrospect, it appears those initial reports failed to control for confounding variables such as antiandrogen withdrawal and hydrocortisone. Suramin causes numerous reversible toxicities (lethargy, rash, fatigue, anemia, hyperglycemia, hypocalcemia, coagulopathies, neutropenia, renal and hepatic complications). Neurotoxicity has been the most significant complication and appears to be related to the intensity of the dosing regimen. An optimal therapeutic dose has not been determined, but it is clear that adaptive controls add little benefit. Aside from moderate toxicities and the low therapeutic index in patients with prostate cancer, Suramin's development has taught us some valuable lessons (i.e., anti-androgen withdrawal was noted during Suramin's development, the use of PSA as an indicator of tumor burden was initiated during the evaluation of Suramin). These lessons can be applied to all clinical trials in hormone refractory prostate cancer. Suramin has significantly enhanced the evolution of our knowledge in several areas of prostate cancer biology and treatment.
Suramin-induced polyneuropathy
Neurology 1990 Jun;40(6):954-60.PMID:2161094DOI:10.1212/wnl.40.6.954.
We report the development of a severe polyneuropathy in 4 of 38 patients who were receiving parenteral Suramin therapy for the treatment of various underlying malignancies. In 2 of these patients, the neuropathy progressed to generalized flaccid paralysis with bulbar and respiratory involvement, requiring endotracheal intubation and ICU monitoring. EMG and nerve conduction studies showed evidence of conduction block, suggestive of a demyelinating polyneuropathy. After several weeks, both patients improved clinically. The other 2 patients developed a reversible neuropathy with flaccid paresis of the limbs but without bulbar or respiratory compromise. No immediate response to plasmapheresis was noted. All 4 patients demonstrated an elevated CSF protein in the acute phase of their neuropathy, which declined or returned to normal during recovery. The development of polyneuropathy correlated with the maximum plasma Suramin level, with an estimated 40% risk of developing neurotoxicity in those patients whose maximum level was 350 micrograms/ml or greater. No correlation could be made with the total dose of Suramin administered or with the duration of therapy. Two of these 4 patients manifested tumor shrinkage while receiving Suramin therapy. We conclude that Suramin, a promising antineoplastic agent, is capable of inducing a severe sensorimotor polyneuropathy which appears to be related to the plasma concentration of Suramin. Serial measurement of the plasma concentration during Suramin therapy is recommended.
1984-Discovery of the First Anti-HIV Drug, Suramin
Viruses 2021 Aug 19;13(8):1646.PMID:34452510DOI:10.3390/v13081646.
In 2021, we commemorate the 40th anniversary of the identification of the disease AIDS, the acquired immune deficiency syndrome, a name that for the first time in history was launched in 1981 [...].
Suramin: clinical uses and structure-activity relationships
Mini Rev Med Chem 2008 Nov;8(13):1384-94.PMID:18991754DOI:10.2174/138955708786369573.
Suramin is a polysulfonated polyaromatic symmetrical urea. It is currently used to treat African river blindness and African sleeping sickness. Suramin has also been extensively trialed recently to treat a number of other diseases, including many cancers. Here, we examine its modes of action and discuss its structure-activity relationships.
Suramin: potential in acute liver failure
Expert Opin Investig Drugs 2004 Oct;13(10):1361-3.PMID:15461564DOI:10.1517/13543784.13.10.1361.
Apoptosis is the first cellular response of the liver to many toxic events, including viral hepatitis, alcohol-induced liver disease and ischaemia/reperfusion injury. When apoptosis is induced with an antibody to APO-1, Suramin is antiapoptotic in a variety of cell lines (e.g., Jurkat cells, HepG2). Jo2 is an antibody to mouse CD95, which kills C57Bl/6 mice, and was used as a model of fulminant liver failure in mice. Suramin protected 40% of Jo2-treated mice from death and delayed death in the other mice. In mice, D-galactosamine and endotoxin cause apoptotic liver damage, which is mediated by TNF. Suramin reduced this liver damage as assessed by serum aminotransferase levels, gross liver appearance and apoptosis levels. In contrast, Suramin does not inhibit necrotic cell death in a rat model of liver transplantation. Inhibition of apoptosis with Suramin or other more selective agents is an approach that should be further investigated in liver failure.