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Topotecan

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Chemical Structure| 123948-87-8 同义名 : 拓扑替康盐酸盐水合物 ;NSC 609669;SKF 104864A
CAS号 : 123948-87-8
货号 : A144786
分子式 : C23H23N3O5
纯度 : 98%
分子量 : 421.446
MDL号 : MFCD00870670
存储条件：

粉末 Sealed in dry,Store in freezer, under -20°C

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 105 mg/mL(249.14 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
动物实验配方：
生物活性
靶点

  • Topo I

    Topo I (MCF-7 Luc cells), IC50:13 nM

    Topo I (DU-145 Luc cells), IC50:2 nM
描述 Topotecan is a potent anti-cancer (antineoplastic or cytotoxic) chemotherapy drug. This medication is classified as a topoisomerase 1 inhibitor. Topotecan is used to treat cancer of the ovaries when other treatments have failed, and at the same time, it may also be used to against small- cell and non-small-cell lung cancer, breast cancer, and acute leukemia[3]. The cytotoxicity of topotecan in vitro is related to exposure time and is significantly greater with continuous exposure to low concentrations of the drug than brief exposure to higher concentrations. Topotecan exhibited some selectivity for human ovarian tumour cells in vitro. Intraperitoneal administration of topotecan 10 mg/kg once every 4 days increased median survival time in mice with an intraperitoneal human ovarian cancer xenograft[4].
临床研究
NCT号 适应症或疾病 临床期 招募状态 预计完成时间 地点
NCT00259935 Lung Cancer, Small Cell Phase 1 Completed - United States, New Hampshire ... 展开 >> GSK Investigational Site Lebanon, New Hampshire, United States, 03756 United States, New York GSK Investigational Site Bronx, New York, United States, 10461 United States, Pennsylvania GSK Investigational Site Philadelphia, Pennsylvania, United States, 19111 United States, Tennessee GSK Investigational Site Nashville, Tennessee, United States, 37203 United States, Texas GSK Investigational Site San Antonio, Texas, United States, 78229 United States, West Virginia GSK Investigational Site Morgantown, West Virginia, United States, 26506 Netherlands GSK Investigational Site Amsterdam, Netherlands, 1066 CX GSK Investigational Site Utrecht, Netherlands, 3584 CX 收起 <<
NCT00502762 Lung Cancer R... 展开 >>efractory to Chemotherapy 收起 << Phase 2 Unknown August 2007 Korea, Republic of ... 展开 >> Gachon University Gil Medical Center Incheon, Korea, Republic of, 405 760 收起 <<
NCT01039025 Myeloma Phase 2 Completed - United States, Texas ... 展开 >> U.T. M.D. Anderson Cancer Center Houston, Texas, United States, 77030 收起 <<
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.37mL

0.47mL

0.24mL

11.86mL

2.37mL

1.19mL

23.73mL

4.75mL

2.37mL
参考文献

[1]Zhang FL, Wang P, et al. Topoisomerase I inhibitors, shikonin and topotecan, inhibit growth and induce apoptosis of glioma cells and glioma stem cells. PLoS One. 2013 Nov 26;8(11):e81815.

[2]Kumar S, Mokhtari RB, et al. Metronomic oral topotecan with pazopanib is an active antiangiogenic regimen in mouse models of aggressive pediatric solid tumor. Clin Cancer Res. 2011 Sep 1;17(17):5656-67.

[3]Saraf S, Jain A, Hurkat P, Jain SK. Topotecan Liposomes: A Visit from a Molecular to a Therapeutic Platform. Crit Rev Ther Drug Carrier Syst. 2016;33(5):401-432.

[4]Brogden RN, Wiseman LR. Topotecan. A review of its potential in advanced ovarian cancer. Drugs. 1998;56(4):709-723.