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Topotecan

Catalog No. T5784   CAS 123948-87-8
Synonyms: NSC 609669, SKF 104864A

Topotecan (NSC-609669) is a Topoisomerase I inhibitor,and is an antineoplastic agent used to treat ovarian cancer that works by inhibiting DNA topoisomerases.

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Topotecan Chemical Structure
Topotecan, CAS 123948-87-8
Pack Size Availability Price/USD Quantity
5 mg In stock $ 32.00
10 mg In stock $ 50.00
25 mg In stock $ 82.00
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Purity: 95.19%
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Biological Description
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Storage & Solubility Information
Description Topotecan (NSC-609669) is a Topoisomerase I inhibitor,and is an antineoplastic agent used to treat ovarian cancer that works by inhibiting DNA topoisomerases.
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[1].
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[2].
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[1].
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[2].
Source
Synonyms NSC 609669, SKF 104864A
Molecular Weight 421.45
Formula C23H23N3O5
CAS No. 123948-87-8

Storage

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

Solubility Information

DMSO: 84 mg/mL (199.31 mM)

TargetMolReferences and Literature

1. Feng-Lei Z , Ping W , Yun-Hui L , et al. Topoisomerase I Inhibitors, Shikonin and Topotecan, Inhibit Growth and Induce Apoptosis of Glioma Cells and Glioma Stem Cells[J]. PLoS ONE, 2013, 8(11):e81815-. 2. Taich P , Moretton M A , Del Sole, María Jose, et al. Sustained-release hydrogels of topotecan for retinoblastoma[J]. Colloids and Surfaces B: Biointerfaces, 2016, 146:624-631. 3. Zeng X, Zhu S, Lu W, et al. Target identification among known drugs by deep learning from heterogeneous networks[J]. Chemical Science. 2020, 11(7): 1775-1797.

TargetMolCitations

1. Zeng X, Zhu S, Lu W, et al. Target identification among known drugs by deep learning from heterogeneous networks. Chemical Science. 2020, 11(7): 1775-1797. 2. Zeng H, Xie H, Ma Q, et al.Identification of N-(3-(methyl (3-(orotic amido) propyl) amino) propyl) oleanolamide as a novel topoisomerase I catalytic inhibitor by rational design, molecular dynamics simulation, and biological evaluation.Bioorganic Chemistry.2023: 106734.

Related compound libraries

This product is contained In the following compound libraries:
Anti-Cancer Approved Drug Library Anti-Cancer Drug Library Anti-Cancer Clinical Compound Library Anti-Cancer Active Compound Library FDA-Approved & Pharmacopeia Drug Library DNA Damage & Repair Compound Library Natural Product Library Bioactive Compound Library Human Metabolite Library Bioactive Compounds Library Max

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Related compounds with same targets
1,4-Naphthoquinone EIDD-1931 3-Hydroxysarpagine Irinotecan hydrochloride trihydrate NU2058 Genz-644282 Rebeccamycin Teniposide

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Keywords

Topotecan 123948-87-8 Autophagy DNA Damage/DNA Repair Topoisomerase orally active NSC-609669 NSC609669 NSC 609669 GSCs-U251 inhibit U87 Inhibitor U251 SKF 104864A GSCs-U87 inhibitor

 

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