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Topotecan HCl

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Chemical Structure| 119413-54-6 同义名 : 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
CAS号 : 119413-54-6
货号 : A122669
分子式 : C23H24ClN3O5
纯度 : 98%
分子量 : 457.91
MDL号 : MFCD00866235
存储条件:

粉末 Sealed in dry,Room Temperature

液体 -20°C:3-6个月-80°C:12个月

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

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].
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
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 - -
实验方案
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

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.