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Topotecan HCl.

(Synonyms: 盐酸拓扑替康; SKF 104864A hydrochloride; NSC 609669 hydrochloride)

目录号: PC10355 纯度: ≥98%

Topotecan Hydrochloride (SKF 104864A; NSC 609669) 是具有抗癌活性的拓扑异构酶I 抑制剂。

CAS No. :119413-54-6

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PC10355-10mM (in 1mL DMSO)	10mM (in 1mL DMSO)	¥700.00	请登录

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中文名称	Topotecan HCl.
中文别名	盐酸拓扑替康;盐酸拓盐酸拓扑替坎;盐酸拓扑特康;盐酸拓普替康;托泊替康;拓扑替康;拓扑替康盐酸盐;拓普替康;盐酸拓扑替康(P);盐酸拓扑替康,Topotecan HCl,植物提取物,标准品,对照品;盐酸拓扑替康标准品;盐酸拓扑替康,Topotecan hydrochloride,对照品,标准品,中草药;(S)-10-[(二甲基氨基)甲基]-4-乙基-4,9-二羟基-1H-吡喃并[3',4':6,7]中氮茚并[1,2-b]-喹啉-3-14(4H,12H)-二酮盐酸盐;盐酸拓扑替;拓扑替康(盐酸);盐酸拓普替康(替康类);拓扑替康盐酸盐(标准品);TOPOTECAN HYDROCHLORIDE 盐酸拓扑替康;盐酸拓扑替康 1G
英文名称	Topotecan HCl
英文别名	Topotecan Hydrochloride;(S)-10-[(Dimethylamino)methyl]-4-ethyl-4,9-dihydroxy-1H-pyrano[3',4':6,7]indolizino[1,2-b]quinoline-3,14(4H,12H)-dione monohydrochloride;Nogitecan hydrochloride;Hycamtin;Topotecan HCl;Topotecan (hydrochloride);TOPOTECAN HCL(P)(CALL);Topotecan Hydrochlor;Topotecan, hydrochloride Salt (NSC 609699,SK&F 104864-A,Hycamtin®);NSC 609669;SK&F 104864-A;SKF 104864A;SKFS 104864A;SKF-104864A;Levulan-13C;HYDROCHLORIDE;Nogitecan HCl;5-ALA HCl-13C;SKF-S 104864-A;Hycamptamine hydrochloride;Topotecan monohydrochloride;Topotecan hydrochloride [USAN];NSC609699;956S425ZCY;Hycamtin (TN);DSSTox_RID_81248;DSSTox_CID_2;DSSTox_CID_25952;DSSTox_GSID;7M7YKX2N15;hycamptamine hydrochloride hydrate;NSC-609669 hydrochloride hydrate;SKF-104864A hydrochloride hydrate;Topotecan;Topotecane;Topotecanum;Hycamptin;Topotecan lactone;TpT;(S)-10-((Dimethylamino)methyl)-4-ethyl-4,9-dihydroxy-1H-pyrano(3',4':6,7)indolizino(1,2-b)quinoline-3,14(4H,12H)-dione;119413-54-6 (HCL);123948-87-8 (free base);1H-Pyrano(3',4':6,7)indolizino(1,2-b)quinoline-3,14(4H,12H)-dione, 10-((dimethylamino)methyl)-4-ethyl-4,9-dihydroxy-, (S)-;9-Dimethylaminomethyl-10-hydroxycamptothecin;BSPBio_002348;dihydroxy(oxo)silane; dioxido(dioxo)molybdenum;HSCI1_000228;https://www.ebi.ac.uk/chebi/searchId.do?chebiId=CHEBI:63632;Hycamptamine;Hycamtamine;Hycamtin®;Hycamtin®\|SK-S-104864-A;Hycamtin;SKF104864;MLS000759456;SKF104864;SKF-S 104864;SK-S-104864-A;SMP2_000312;SMP2_000327;Topotecan hydrochloride hydrate;Topotecan-d5;Topotecan-d6;Topotecane; Topotecanum;TTC;UNII:7M7YKX2N15;UNII-7M7YKX2N15
Cas No.	119413-54-6
分子式	C₂₃H₂₃N₃O₅
分子量	421.45
包装储存	4°C, sealed storage, away from moisture and light *In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)
详情描述	Topotecan Hydrochloride (SKF 104864A; NSC 609669) 是具有抗癌活性的拓扑异构酶I 抑制剂。

生物活性

Topotecan Hydrochloride (SKF 104864A Hydrochloride) is a Topoisomerase I inhibitor with potent antineoplastic activities.

性状

Solid

IC50 & Target[1][2]

Topoisomerase I

体外研究(In Vitro)

Topotecan Hydrochloride (SKF 104864A Hydrochloride) obviously inhibits proliferation of not only human glioma cells but also glioma stem cells (GSCs) in a dose- and time-dependent manner. According to the IC₅₀ values at 24 h, 3 μM of Topotecan Hydrochloride is selected as the optimal administration concentration. In addition, Topotecan Hydrochloride induces cell cycle arrest in G0/G1 and S phases and promoted apoptosis. Results show that the cell viability is inhibited by Topotecan Hydrochloride in a dose-dependent manner. 2, 20 and 40 μM of Topotecan Hydrochloride obviously inhibits the cell viability compared with the control groups. The IC₅₀ values of Topotecan Hydrochloride at 24 h are 2.73±0.25 μM of U251 cells, 2.95±0.23 μM of U87 cells, 5.46±0.41 μM of GSCs-U251 and 5.95±0.24 μM of GSCs-U87. Thus 3 μM of Topotecan Hydrochloride is selected as the optimal administration concentration in the subsequent experiments.

Medlife has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究(In Vivo)

NUB-7 metastatic model, the animals belonging to all the 4 groups are sacrificed after 14 days treatment. Compared with the control, Low dose metronomic (LDM) Topotecan Hydrochloride and TP+Pazopanib (PZ) liver weights are significantly lower in TP+PZ-treated animals, compared with PZ. Microscopic tumors are visible in the livers of mice belonging to all the groups except TP+PZ confirming the ability of Topotecan Hydrochloride+PZ to control liver metastasis. In a previous dose-response study, the daily dose of oral metronomic Topotecan Hydrochloride (0.5, 1.0, and 1.5 mg/kg) causes greater reduction in microvascular density compared with weekly maximum-tolerated dose regimen (7.5 and 15 mg/kg) in an ovarian cancer model, but the mice treated with 1.5 mg/kg daily, oral Topotecan Hydrochloride show decreased food intake, and a lesser antitumor effect.

Medlife has not independently confirmed the accuracy of these methods. They are for reference only.

运输条件

Room temperature or refrigerated transportation.

储存方式

4°C, sealed storage, away from moisture and light

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)

ClinicalTrial

结构分类

来源

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. [Information]

[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. [Information]

溶解度数据

体外研究:

DMSO : 100 mg/mL (218.38 mM; Need ultrasonic)

H₂O : 33.33 mg/mL (72.79 mM; Need ultrasonic)

配制储备溶液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	2.1838 mL	10.9192 mL	21.8384 mL
5 mM	0.4368 mL	2.1838 mL	4.3677 mL
10 mM	0.2184 mL	1.0919 mL	2.1838 mL

产品不同，其溶解度不同。建议根据产品选择合适的溶剂配制储备溶液；配成溶液后，建议分装保存，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, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)。-80°C 储存时，建议在 6 个月内使用，-20°C 储存时，建议在 1 个月内使用。

体内研究:

建议根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都建议先按照 体外研究 方式配制澄清的储备液，再依次添加助溶剂：

——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用；以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

1.

建议依照次序添加每种溶剂： 10% DMSO 90% corn oil
Solubility: ≥ 2.5 mg/mL (5.46 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (5.46 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。
以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。
2.

建议依照次序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% saline
Solubility: ≥ 2.08 mg/mL (4.54 mM); Clear solution

此方案可获得 ≥ 2.08 mg/mL (4.54 mM，饱和度未知) 的澄清溶液。
以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。
将 0.9 g 氯化钠，完全溶解于 100 mL ddH?O 中，得到澄清透明的生理盐水溶液
3.

建议依照次序添加每种溶剂： 10% DMSO 90% (20% SBE-β-CD in saline)
Solubility: ≥ 2.08 mg/mL (4.54 mM); Clear solution

此方案可获得 ≥ 2.08 mg/mL (4.54 mM，饱和度未知) 的澄清溶液。
以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。
将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中，再用生理盐水定容至 10 mL，完全溶解，澄清透明

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产品使用指南

Data Sheet

1：一般建议：溶解度为Medlife测试数据，可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解，请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异，仅做参考，具体以实验方案为准。

2：储存条件：粉末-20°C一般情况可以保存3年，溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异，请细致阅读产品信息，并辅助参考相关文献描述。

Topotecan HCl.

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