Topotecan HCl

Catalog No.S1231 Synonyms: NSC609699, Nogitecan HCl, SKFS 104864A

Topotecan HCl Chemical Structure

Molecular Weight(MW): 457.91

Topotecan HCl is a topoisomerase I inhibitor for MCF-7 Luc cells and DU-145 Luc cells with IC50 of 13 nM and 2 nM in cell-free assays, respectively.

Size Price Stock Quantity  
In DMSO USD 230 In stock
USD 180 In stock
USD 320 In stock

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2 Customer Reviews

  • Cells were treated at the same concentrations as in Caspase3/7 assay for 16 hours and total cell lysates were prepared for Western blotting. GAPDH was used as a loading control.

    BMC Cancer, 2015, 10.1186/s12885-015-1231-z. Topotecan HCl purchased from Selleck.

    Pax3:Foxo1a knockdown increases select chemotherapy sensitivities. MTS assay was performed for Pax3:Foxo1a knockdown mouse aRMS tumor cells treated with DNA damaging agents and microtubule inhibitors. Pax3:Foxo1a knockdown reduced the concentration at which viability was impaired by 50% (IC50) of topotecan by 4.8 fold, respectively, yet did not affect the IC50 of mafosfamide.

    PLoS Genet 2014 10(1), e1004107. Topotecan HCl purchased from Selleck.

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Notes:

2. For more details, such as half maximal inhibitory concentrations (IC50s) and working concentrations of each inhibitor, please click on the link of the inhibitor of interest.
3. "+" indicates inhibitory effect. Increased inhibition is marked by a higher "+" designation.
4. Orange "√" refers to compounds which do inhibitory effects on the related isoform, but without specific value.

Biological Activity

Description Topotecan HCl is a topoisomerase I inhibitor for MCF-7 Luc cells and DU-145 Luc cells with IC50 of 13 nM and 2 nM in cell-free assays, respectively.
Features Topotecan is a water-soluble derivative of camptothecin.
Targets
Topo I (DU-145 Luc cells) [1]
(Cell-free assay)
Topo I (MCF-7 Luc cells) [1]
(Cell-free assay)
2 nM 13 nM
In vitro

Stronger drug activity of Topotecan is observed for DU-145 Luc and MCF-7 Luc cells. [1] Topotecan causes cytotoxicity during the course of DNA replication by stabilizing the covalent complex between topoisomerase I and DNA and preventing the religation of enzyme-linked single-strand DNA break. Topotecan stabilizes topoisomerase I/DNA cleavable complexes in radiation-resistant human B-lineage acute lymphoblastic leukemia (ALL) cells, causes rapid apoptotic cell death despite high-level expression of bcl-2 protein, and inhibits ALL cell clonogenic growth in a dose-dependent fashion. [2]

In vivo Animals inoculate s.c. with DU-145 Luc cells and then treated with Topotecan demonstrates significant tumor growth and regression as measured with calipers and luminescent imaging. The correlation coefficient is 0.75 for the control untreated group and 0.93 for the Topotecan-treated group. Similarly, tumor progression and regression are measurable using luminescent imaging for untreated and Topotecan-treated mice inoculated i.p. with MCF-7 Luc cells. [1] Topotecan elicited potent antileukemic activity in severe combined immune-deficiency (SCID) mouse models of human poor prognosis ALL. Topotecan markedly improved event-free survival of SCID mice challenged with otherwise fatal doses of humaln leukemia cells at systemic drug exposure levels. [2] Gliomas preferentially express TRAIL R2 and that treatment with Topotecan significantly up-regulates its expression. [3]

Protocol

Cell Research:

[1]

+ Expand
  • Cell lines: MCF-7 Luc and DU-145 Luc cells
  • Concentrations: 0 μg/mL - 0.692 μg/mL
  • Incubation Time: 96 hours
  • Method:

    Topotecan is dissolved in sterile water to a stock concentration of 1 mg/mL, diluted to 6 μg/mL in cultured medium and then serially diluted 1:4 in opaque, white tissue culture-treated microplates to a final volume of 0.1 mL/well. MCF-7 Luc and DU-145 Luc cells are resuspended in 3×104 cells/mL in DMEM with high glucose containing 10% FBS and 0.5 mg/mL Geneticin; 100 μL of cells are added in each well. Plates are incubated for 4 days at 37 °C in 95% humidity/5% CO2. After incubation, 0.05 mL of 0.1 M HEPES buffer (pH 7.9) containing 50 μg/mL D-luciferin is added to each well. After incubation at room temperature for 10 minutes, the culture microplate is measured in a microplate luminometer and a molecular light imager. Results obtained with the microplate luminometer are calculated using no inhibition control wells without exogenous drug and maximum inhibition control wells containing ATP inhibitor. Results for the molecular light imager are similarly calculated using values obtained with a 5 minutes luminescent imager.


    (Only for Reference)
Animal Research:

[1]

+ Expand
  • Animal Models: Mice with MCF-7 Luc or DU-145 Luc cells
  • Formulation: PBS
  • Dosages: 0.25 mg/mL
  • Administration: Administered via i.p.
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 92 mg/mL (200.91 mM)
Water 92 mg/mL (200.91 mM)
Ethanol <1 mg/mL
In vivo Saline 30 mg/mL

* 1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 457.91
Formula

C23H23N3O5.HCl

CAS No. 119413-54-6
Storage powder
in solvent
Synonyms NSC609699, Nogitecan HCl, SKFS 104864A

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Clinical Trial Information

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT00553189 Completed Solid Tumors|Lymphomas National Cancer Institute (NCI)|National Institutes of Health Clinical Center (CC) August 9, 2007 Phase 1
NCT00117013 Completed Neoplasms National Cancer Institute (NCI)|National Institutes of Health Clinical Center (CC) June 28, 2005 Phase 1
NCT02980809 Not yet recruiting Small Cell Lung Cancer First Hospitals affiliated to the China PLA General Hospital March 2017 Phase 2
NCT02963090 Not yet recruiting Small Cell Lung Cancer Alliance Foundation Trials, LLC.|Merck Sharp & Dohme Corp. December 2016 Phase 2
NCT02348398 Withdrawn Cervical Cancer M.D. Anderson Cancer Center|GlaxoSmithKline August 2016 Phase 2
NCT02822157 Not yet recruiting Ovarian Epithelial Cancer Universitaire Ziekenhuizen Leuven|AstraZeneca August 2016 Phase 2

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Topoisomerase Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID