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Topotecan HCl

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Catalog No.
B2296
Topoisomerase 1(拓扑异构酶 1)抑制剂
组合的产品项目
规格价格库存 数量
10mM (in 1mL DMSO)
¥ 550.00
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10mg
¥ 400.00
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50mg
¥ 1,300.00
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100mg
¥ 1,500.00
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Background

Topotecan HCl(SKF104864)is an inhibitor of topoisomerase 1 and semisynthetic analogue of camptothecin [1].

Topotecan HCl(SKF104864)has been reported to have a potent antitumor activity against tumors in murine models. In addition, Topotecan HCl has also shown the potent effect against intravenously implanted P388 leukemia and both intravenously and subcutaneously implanted Lewis lung carcinoma. Topotecan HCl has noted the activity against subcutaneously implanted solid tumors including chemorefractory tumors and human colon carcinoma xenograft HT-29. Topotecan HCl has been found to induce regressions in the lung tumor model (Lewis lung carcinoma and B16 melanoma), compared to camptothecin and 9-amino-camptothecin. In the preclinical toxicology studies, Topotecan HCl has been revealed to have a concentration-dependent, reversible and limited toxoicity to rapidly proliferation tissues such as bone marrow and gastro-intestinal epithelium [1].

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

Chemical Properties

Physical AppearanceA solid
StorageStore at -20°C
M.Wt457.91
Cas No.119413-54-6
FormulaC23H24ClN3O5
Solubility≥22.9mg/mL in DMSO
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 hydrochloride
SDFDownload SDF
Canonical SMILESCl[H].O=C1N(C([H])([H])C2=C([H])C(C(C([H])([H])N(C([H])([H])[H])C([H])([H])[H])=C3O[H])=C(C([H])=C3[H])N=C42)C4=C([H])C([C@@](C([H])([H])C([H])([H])[H])5O[H])=C1C([H])([H])OC5=O
运输条件试用装:蓝冰运输。 其他可选规格:常温运输或根据您的要求用蓝冰运输。
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。

试验操作

细胞实验:

细胞系

MCF-7乳腺癌细胞系、人前列腺癌细胞系(PC-3和LNCaP)

溶解方法

该化合物在DMSO中的溶解度 > 10 mM。若配制更高浓度的溶液,一般步骤如下:请将试管置于37℃加热10分钟和/或将其置于超声波浴中震荡一段时间。原液于-20℃可放置数月。

反应时间

500 nM、持续6-12天; 或2、10 nM,持续72小时

应用

Topotecan处理的细胞在体外显示受损的球形成能力。Topotecan处理MCF-7细胞诱导的ABCG2表达与CD24/EpCAM表达降低相关[1]。此外,Topotecan以浓度依赖性方式增加PC-3和LNCaP细胞毒性 [2]。

动物实验:

动物模型

新生的NOD.Cg-Prkdcscid Il2rgtm1Wjl/SzJ (NSG)小鼠或成年NMRI-nu/nu小鼠模型; PC-3异种移植模型

剂量

2.45和0.10 mg/kg/天、肿瘤内注射、连续输注或常规尾静脉注射给药,30天

应用

Topotecan处理的细胞降低免疫缺陷小鼠的致瘤性 [1]。 此外,低剂量连续给予Topotecan可增强前列腺癌的抗肿瘤活性 [2]。

注意事项

请于室内测试所有化合物的溶解度。实际溶解度和理论值可能略有不同,这是由实验系统的误差引起的,属于正常现象。

References:

1. Huber, S., Wege, A. K., Bernhardt, G., Buschauer, A. and Brockhoff, G. (2015) Topotecan-induced ABCG2 expression in MCF-7 cells is associated with decreased CD24 and EpCAM expression and a loss of tumorigenicity. Cytometry A. 87, 707-716

2. Aljuffali, I. A., Mock, J. N., Costyn, L. J., Nguyen, H., Nagy, T., Cummings, B. S. and Arnold, R. D. (2011) Enhanced antitumor activity of low-dose continuous administration schedules of topotecan in prostate cancer. Cancer Biol Ther. 12, 407-420

质量控制

化学结构

Topotecan HCl