| Suramin hexasodium salt 目录号 GC16832 |
Sample solution is provided at 25 µL, 10mM.
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Purity: >98.00%
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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]. |
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. | |
| Cas No. | 129-46-4 | SDF | |
| 别名 | N/A | ||
| 化学名 | sodium 8,8'-((3,3'-((3,3'-(carbonylbis(azanediyl))bis(benzoyl))bis(azanediyl))bis(4-methylbenzoyl))bis(azanediyl))bis(naphthalene-1,3,5-trisulfonate) | ||
| Canonical SMILES | [O-]S(=O)(C1=C(C(NC(C2=CC=C(C)C(NC(C3=CC=CC(NC(NC4=CC(C(NC5=CC(C(NC(C(C6=CC(S([O-])(=O)=O)=C7)=C7S([O-])(=O)=O)=CC=C6S([O-])(=O)=O)=O)=CC=C5C)=O)=CC=C4)=O)=C3)=O)=C2)=O)=CC=C8S([O-])(=O)=O)C8=CC(S([O-])(=O)=O)=C1)=O.[Na+].[Na+].[Na+].[Na+].[Na+].[Na+] | ||
| 分子式 | C51H34N6Na6O23S6 | 分子量 | 1429.15 |
| 溶解度 | ≥ 71.45mg/mL in H2O | 储存条件 | Store at RT |
| General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while. | ||
| Shipping Condition | Evaluation sample solution : ship with blue ice All other available size: ship with RT , or blue ice upon request |
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Suramin is a polysulfonated naphthylurea that inhibits the binding of calmodulin to recognition sites on the ryanodine receptor-1 (IC50 = 4.9 μM), blocks G protein coupling to GPCRs, and non-selectively antagonizes P2 purinergic receptors (10-100 μM).[1],[2[ Suramin also acts as a non-specific competitor of glycosaminoglycan binding to a variety of targets including TGFβ, PDGF, and FGF and additionally inhibits insulin-like growth factor-l, EGF, PKC activity, TNF, IL-2, transferrin, and Apo-B.[3] While originally used as an early stage treatment of trypanosome-caused onchocerciasis (African river blindness) and African trypanosomiasis (African sleeping sickness), suramin has been under clinical evaluation for its potential to regress a number of cancer cell lines, including non-small cell lung cancer, advanced breast cancer, hormone refractory prostate cancer, metastatic renal cell cancer, colorectal cancer, and high-grade gliomas.[3],[4],[5]
Reference:
[1]. Klinger, M., Bofill-Cardona, E., Mayer, B., et al. Suramin and the suramin analogue NF307 discriminate among calmodulin-binding sites Biochemistry Journal 355(3), 827-833 (2001).
[2]. Charlton, S.J., Brown, C.A., Weisman, G.A., et al. PPADS and suramin as antagonists at cloned P2Y- and P2U- purinoceptors British Journal of Pharmacology 118(3), 704-710 (1996).
[3]. Eisenberger, M.A., and Reyno, L.M. Suramin Cancer Treatment Reviews 20, 259-273 (1994).
[4]. Stein, C.A. Suramin: A novel antineoplastic agent with multiple potential mechanisms of action Cancer Research 53, 2239-2248 (1993).
[5]. McGeary, R.P., Bennett, A.J., Tran, Q.B., et al. Suramin: Clinical uses and structure-activity relationships Mini Rev.Med.Chem. 8(13), 1384-1394 (2008).