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拓扑替康 /Topotecan {[allProObj[0].p_purity_real_show]}

货号:A144786 同义名: 拓扑替康盐酸盐水合物 / NSC 609669;SKF 104864A

Topotecan is an inhibitor of topoisomerase I and the IC50 values in cancer cells are less than 6 μM.

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Type HazMat fee for 500 gram (Estimated)
Excepted Quantity USD 0.00
Limited Quantity USD 15-60
Inaccessible (Haz class 6.1), Domestic USD 80+
Inaccessible (Haz class 6.1), International USD 150+
Accessible (Haz class 3, 4, 5 or 8), Domestic USD 100+
Accessible (Haz class 3, 4, 5 or 8), International USD 200+
Topotecan 化学结构 CAS号:123948-87-8
Topotecan 化学结构
CAS号:123948-87-8
Topotecan 3D分子结构
CAS号:123948-87-8
Topotecan 化学结构 CAS号:123948-87-8
Topotecan 3D分子结构 CAS号:123948-87-8
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Topotecan 纯度/质量文件 产品仅供科研

货号:A144786 标准纯度: {[allProObj[0].p_purity_real_show]}
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产品名称 Topo I Topo II Topo IV Topoisomerase 其他靶点 纯度
Ellagic acid 98%
β-Lapachone 99%+
(s)-10-hydroxycamptothecin 98+%
Camptothecin ++

Topo I, IC50: 0.68 μM

98%
Betulinic acid ++

Eukaryotic topoisomerase I, IC50: 5 μM

98%
Topotecan ++++

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

Topo I (DU-145 Luc cells), IC50: 2 nM

98%
Irinotecan HCl Trihydrate 98%
SN-38 98%
Levofloxacin hydrate 98%
Dexrazoxane 99%+
Ofloxacin 98+%
Enoxacin 99%+
Flumequine +

Topo II, IC50: 15 μM

98%
Levofloxacin 97%
Etoposide 98%
Pefloxacin mesylate dihydrate 99+%
Marbofloxacin 98+%
Voreloxin HCl 98%
Mitoxantrone dihydrochloride PKC 98%
Nalidixic acid 98%
Doxorubicin 98%
Novobiocin sodium 95%
Amonafide 99%+
Pirarubicin 98%+
Idarubicin HCl +++

Topo II (MCF-7 cells), IC50: 3.3 ng/mL

99%+
Genistein EGFR 98%
Teniposide 98%
Moxifloxacin 98%
Ciprofloxacin 98%
Clinafloxacin 97%
Gatifloxacin 98%
Daunorubicin HCl +++

DNA synthesis, Ki: 20 nM

98%
Epirubicin HCl 99%+
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多,抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用,但抑制强度暂时没有相关数据。

Topotecan 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].

Topotecan 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 <<

Topotecan 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.

Topotecan 实验方案

计算器
存储液制备 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

Topotecan 技术信息

CAS号123948-87-8
分子式C23H23N3O5
分子量 421.446
别名 拓扑替康盐酸盐水合物 ;NSC 609669;SKF 104864A
运输蓝冰
存储条件

液体 -20°C:3-6个月-80°C:12个月

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

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

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