Topotecan

SKU: orb1301493

Description

Topotecan (NSC-609669) is a small molecule antineoplastic agent that functions as a Topoisomerase I inhibitor. It is widely used in oncology research, particularly for studying ovarian cancer, and is applied in both in vitro cell-based assays and in vivo xenograft models to investigate its mechanism and efficacy.

Research Area

Cell Biology, Molecular Biology, Pharmacology & Drug Discovery

Key Properties

• CAS Number: 123948-87-8
• MW: 421.45
• Purity: 98.00% (May vary between batches)
• Formula: C₂₃H₂₃N₃O₅
• SMILES: CC[C@@]1(O)C(=O)OCc2c1cc1-c3nc4ccc(O)c(CN(C)C)c4cc3Cn1c2=O
• Target: Topoisomerase|||Autophagy
• Solubility: 10% DMSO+40% PEG300+5% Tween 80+45% Saline:3.3 mg/mL (7.83 mM);DMSO:84 mg/mL (199.31 mM)

Bioactivity

• In Vivo:
  Topotecan-hydrogels can deliver sustained concentrations of active drug into the vitreous with excellent biocompatibility in vivo and pronounced cytotoxic activity in retinoblastoma cells and may become an additional strategy for intraocular retinoblastoma treatment.
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• In Vitro:
  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.
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• Cell Research:
  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.
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• Animal Research:
  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.
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Storage & Handling

• Storage: -20°C
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

Autophagy, inhibit, NSC 609669, orally active, NSC609669, NSC-609669, Inhibitor, Eukaryotic topoisomerase I, GSCs-U251, GSCs-U87, Topoisomerase, Topotecan, SKF 104864A, U251, U87

Compound Identifiers

PubChem CID

60700