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拓扑替康盐酸盐 /Topotecan HCl {[allProObj[0].p_purity_real_show]}

货号:A122669 同义名: 盐酸拓扑替康 / SKF 104864A hydrochloride;NSC 609669 hydrochloride

Topotecan HCl(SKF 104864A Hydrochloride)作为一种拓扑异构酶I抑制剂,具有强效抗肿瘤活性。

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There will be a HazMat fee per item when shipping a dangerous goods. The HazMat fee will be charged to your UPS/DHL/FedEx collect account or added to the invoice unless the package is shipped via Ground service. Ship by air in Excepted Quantity (each bottle), which is up to 1g/1mL for class 6.1 packing group I or II, and up to 25g/25ml for all other HazMat items.

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 HCl 化学结构 CAS号:119413-54-6
Topotecan HCl 化学结构
CAS号:119413-54-6
Topotecan HCl 3D分子结构
CAS号:119413-54-6
Topotecan HCl 化学结构 CAS号:119413-54-6
Topotecan HCl 3D分子结构 CAS号:119413-54-6
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Topotecan HCl 纯度/质量文件 产品仅供科研

货号:A122669 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 (DU-145 Luc cells), IC50: 2 nM

Topo I (MCF-7 Luc cells), IC50: 13 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 HCl 生物活性

描述 Topotecan Hydrochloride (SKF 104864A Hydrochloride) effectively inhibits the proliferation of human glioma cells and glioma stem cells (GSCs) in a dose- and time-dependent manner. An optimal administration concentration of 3 μM is selected based on IC50 values at 24 h. Topotecan Hydrochloride induces cell cycle arrest in G0/G1 and S phases and promotes apoptosis. Additionally, it inhibits cell viability in a dose-dependent manner [1].
体内研究

In the NUB-7 metastatic model, animals from all four groups are sacrificed after 14 days of treatment. Compared to the control group, low dose metronomic (LDM) Topotecan Hydrochloride and TP+Pazopanib (PZ) result in significantly lower liver weights in TP+PZ-treated animals compared to PZ alone. Microscopic tumors are observed in the livers of mice in all groups except TP+PZ, indicating the ability of Topotecan Hydrochloride+PZ to control liver metastasis. In previous dose-response studies, daily oral metronomic Topotecan Hydrochloride (0.5, 1.0, and 1.5 mg/kg) showed greater reduction in microvascular density compared to weekly maximum-tolerated dose regimen (7.5 and 15 mg/kg) in an ovarian cancer model. However, mice treated with 1.5 mg/kg daily oral Topotecan Hydrochloride exhibited decreased food intake and a lesser antitumor effect [2].

体外研究

Topotecan Hydrochloride (SKF 104864A Hydrochloride) effectively inhibits the proliferation of human glioma cells and glioma stem cells (GSCs) in a dose- and time-dependent manner. An optimal administration concentration of 3 μM is selected based on IC50 values at 24 h. Topotecan Hydrochloride induces cell cycle arrest in G0/G1 and S phases and promotes apoptosis. Additionally, it inhibits cell viability in a dose-dependent manner [1].

Topotecan HCl 细胞研究

细胞系 浓度 检测类型 检测时间 活动说明 数据源
A427 human lung carcinoma Proliferation assay Antiproliferative activity measured against A427 human lung carcinoma, IC50=49 nM 9876111
COR-L23/P cell Cytotoxic assay Cytotoxicity measured using the COR-L23 parental (COR-L23/P) human non small cell lung carcinoma cell line, IC50=13.2 nM 11806724
HeLa cells Growth inhibition assay Growth inhibition of HeLa cells after 4 days, GI50=30 nM 17418582
HT-29 cells Cytotoxic assay Cytotoxicity was determined in vitro in HT-29 cells(colon) of human tumor cell lines by using MTT assay, IC50=25 nM 7853331

Topotecan HCl 动物研究

Dose Rat: 0.23 mg/kg[3] (i.v.), 0.7 mg/kg[4] (i.v.); 0.14 mg/kg, 0.79 mg/kg[4] (inh.); 10 ml/kg[5] (p.o.) Dog: 0.068 mg/kg - 0.2 mg/kg[5] (p.o.) Mice: 0.5 mg/kg - 1.5 mg/kg[6] (p.o.)
Administration i.v., inh., p.o.
Pharmacokinetics
Animal Rats[4]
Dose 0.70 mg/kg
Administration i.v.
T1/2 1.4 h
Tmax 0.083 h
Cmax 474 ng/ml
AUC 481 h·ng/ml

Topotecan HCl 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
NCT00231855 Ovarian Neoplasms ... 展开 >> Uterine Neoplasms 收起 << Phase 2 Completed - United States, New York ... 展开 >> Montefiore Medical Center Bronx, New York, United States, 10461 收起 <<
NCT00466232 Small Cell Carcinoma ... 展开 >> Lung Cancer 收起 << Phase 1 Completed - United States, Minnesota ... 展开 >> Park Nicollet Institute St. Louis Park, Minnesota, United States, 55416 收起 <<
NCT00170625 Ovarian Cancer Phase 1 Phase 2 Completed - -

Topotecan HCl 参考文献

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

[2]Kumar S, 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.

Topotecan HCl 实验方案

计算器
存储液制备 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.18mL

0.44mL

0.22mL

10.92mL

2.18mL

1.09mL

21.84mL

4.37mL

2.18mL

Topotecan HCl 技术信息

CAS号119413-54-6
分子式C23H24ClN3O5
分子量 457.91
别名 盐酸拓扑替康 ;SKF 104864A hydrochloride;NSC 609669 hydrochloride;SKF 104864A;NSC 609669;Topotecan (hydrochloride);NSC 609699;SKFS 104864A;Nogitecan HCl;Topotecan HCl
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,Room Temperature

溶解度

DMSO: 105 mg/mL(229.3 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

H2O: 30 mg/mL(65.52 mM),配合低频超声助溶

动物实验配方

PO 0.5% CMC-Na 33 mg/mL suspension

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