Topotecan

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Topotecan

本产品不向个人销售，仅用作科学研究，不用于任何人体实验及非科研性质的动物实验。

CAS NO:

123948-87-8

包装与价格：

包装	价格(元)
10mM (in 1mL DMSO)	电议
10mg	电议
50mg	电议
100mg	电议

产品介绍

化学性质

Physical Appearance	A solid
Storage	Store at -20°C
M.Wt	421.45
Cas No.	123948-87-8
Formula	C₂₃H₂₃N₃O₅
Solubility	≥21.1 mg/mL in DMSO; insoluble in EtOH; insoluble in H2O
Chemical Name	(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
Canonical SMILES	CC[C@]1(O)C(C=C2C3=NC4=CC=C(O)C(CN(C)C)=C4C=C3CN2C5=O)=C5COC1=O
运输条件	蓝冰运输或根据您的需求运输。
一般建议	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。不同厂家不同批次产品溶解度各有差异，仅做参考。若实验所需浓度过大至产品溶解极限，请添加助溶剂助溶或自行调整浓度。溶液形式一般不宜长期储存，请尽快用完。

资料参考

Topotecan(SKF104864)是拓扑异构酶1的抑制剂,是喜树碱的半合成类似物[1].

Topotecan(SKF104864)在小鼠模型中具有有效的抗肿瘤活性.此外,Topotecan对静脉注射植入的P388白血病和静脉注射及皮下植入的Lewis肺癌也有效.Topotecan对皮下植入的实体瘤,包括耐药肿瘤和人类结肠癌异种移植物HT-29也有抗癌活性.相比喜树碱和9-氨基喜树碱,Topotecan可在肺肿瘤模型(Lewis肺癌和B16黑色素瘤)中诱导肿瘤消退.在临床前毒理学研究中,Topotecan对快速增值的组织如骨髓和胃肠上皮具有浓度依赖的可逆的有限毒性[1].

参考文献：
[1] Creemers GJ1, Lund B, Verweij J. Topoisomerase I inhibitors: topotecan and irenotecan. Cancer Treat Rev. 1994 Jan;20(1):73-96.

试验操作

Cell experiment:[1]
Cell lines	Human glioma cell lines U251, U87, GSCs-U251 and GSCs-U87
Reaction Conditions	0.02, 0.2, 2, 20 or 40 μmol/L topotecan for 12, 24 or 48 h incubation
Applications	Topotecan obviously inhibited proliferation of not only human glioma cells but also glioma stem cells in a dose- and time-dependent manner. In addition, topotecan (3 μmol/L, 24 h) induced cell cycle arrest in G0/G1 and S phases and promoted apoptosis.
Animal experiment:[2]
Animal models	Mouse models of aggressive pediatric solid tumor
Dosage form	1 mg/kg Once daily by oral gavage
Applications	Metronomic administration of topotecan and pazopanib showed a statistically significant antitumor activity compared with respective single agents in pediatric tumor mouse models, representing a valid option as a maintenance therapy in aggressive pediatric solid tumors.
Note	The technical data provided above is for reference only.
	References: 1. Zhang FL, Wang P, Liu YH, et al. Topoisomerase I inhibitors, shikonin and topotecan, inhibit growth and induce apoptosis of glioma cells and glioma stem cells. PLoS One, 2013, 8(11): e81815. 2. Kumar S, Mokhtari RB, Sheikh R, et al. Metronomic oral topotecan with pazopanib is an active antiangiogenic regimen in mouse models of aggressive pediatric solid tumor. Clinical Cancer Research, 2011, 17(17): 5656-5667.