拓扑替康 T5784

Product Introduction
Bioactivity


英文名: Topotecan

描述: Topotecan (NSC-609669) 是一种拓扑异构酶 I 抑制剂，通过抑制 DNA 拓扑异构酶起抗肿瘤作用，可用于治疗卵巢癌。

细胞实验: After isolated and identified the GSCs from glioma cells successfully, U251, U87, GSCs-U251 and GSCs-U87 cells were administrated with various concentrations of shikonin or topotecan at different time points to seek for the optimal administration concentration and time point.?The cell viability, cell cycle and apoptosis were detected using cell counting kit-8 and flow cytometer to observe the inhibitory effects on glioma cells and GSCs[1].

动物实验: Hydrogel cytotoxicity was evaluated in retinoblastoma cells as a surrogate for efficacy and Topotecan vitreous pharmacokinetics and systemic as well as ocular toxicity were evaluated in rabbits. The pseudoplastic behavior of the hydrogels makes them suitable for intraocular administration. In vitro release profiles showed a sustained release of Topotecan from PCL-PEG-PCL up to 7days and drug loading did not affect the release pattern. Blank hydrogels did not affect retinoblastoma cell viability but 0.4% (w/w) Topotecan-loaded hydrogel was highly cytotoxic for at least 7days. After intravitreal injection, Topotecan vitreous concentrations were sustained above the pharmacologically active concentration. One month after injection, animals with blank or Topotecan-loaded hydrogels showed no systemic toxicity or retinal impairment on fundus examination, electroretinographic, and histopathological assessments[2].

体外活性: Topoisomerase I inhibitors, ?topotecan, inhibited growth and induced apoptosis of GSCs as well as glioma cells, which suggested that they might be the potential anticancer agents targeting gliomas to provide a novel therapeutic strategy[1].

体内活性: Topotecan-水凝胶能够向玻璃体持续输送活性药物，具有优良的体内生物相容性以及在视网膜母细胞瘤细胞中明显的细胞毒作用，可能成为眼内视网膜母细胞瘤治疗的一个补充策略[2]。

存储条件: Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度: 5% DMSO+95% Saline : 4.2 mg/mL (9.97 mM, suspension)
DMSO : 84 mg/mL (199.31 mM)


关键字: orally active | NSC-609669 | NSC609669 | GSCs-U251 | inhibit | Topotecan | U87 | Inhibitor | U251 | Autophagy | Topoisomerase | GSCs-U87

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相关库: Drug Repurposing Compound Library | Anti-Cancer Compound Library | Anti-Cancer Drug Library | Anti-Cancer Clinical Compound Library | Inhibitor Library | Anti-Cancer Active Compound Library | Anti-Cancer Approved Drug Library | EMA Approved Drug Library | Chemotherapy Drug Library | Bioactive Compound Library

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注：该产品未在中华人民共和国食品药品监督管理部门申请医疗器械注册和备案，不可用于临床诊断或治疗等相关用途