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Ellipticine

Cat. No. M9023
Ellipticine Structure
Synonym:

CCG36483; NSC71795

Size Price Availability Quantity
10mg USD 135  USD135 In stock
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Quality Control
  • Current batch:
  • Purity >98%
  • COA
  • MSDS
Biological Activity

Ellipticine is a DNA intercalating agent and a DNA topoisomerase II inhibitor. Ellipticine is also a natural product, isolated in 1959 from the Australian evergreen tree of the Apocynaceae family. Ellipticine can act as an inhibitor or inducer of biotransformation enzymes, thereby modulating its own metabolism leading to its genotoxic and pharmacological effects. Treatment of cells with ellipticine results in inhibition of cell growth and proliferation.

In vivo, Ellipticine treatment results in ellipticine-derived DNA adduct generation in several healthy organs and in DNA of mammary adenocarcinoma. The induced expression of cytochrome b5 protein in liver of rats treated with ellipticine suggests that cytochrome b5 may modulate the CYP-mediated bioactivation and detoxification of ellipticine.

Protocol
Cell Experiment
Cell lines MCF-7, U87MG, CCRF-CEM, UKF-NB-3 and UKF-NB-4 neuroblastoma cell lines
Preparation method Cells in exponential growth were seeded at 1×104 per well in a 96-well microplate. After incubation (48 hours) at 37 °C in 5% CO2 saturated atmosphere the MTT solution (2 mg/ml PBS) was added, the microplates were incubated for 4 hours and cells lysed in 50% N,N-dimethylformamide containing 20% of sodium dodecyl sulfate (SDS), pH 4.5. The absorbance at 570 nm was measured for each well by multiwell ELISA reader Versamax (Molecular devices, CA, USA). The mean absorbance of medium controls was subtracted as a background. The viability of control cells was taken as 100% and the values of treated cells were calculated as a percentage of control. The IC50 values were calculated from at least 3 independent experiments using linear regression of the dose-log response curves by SOFTmaxPro.
Concentrations 0, 0.1, 1, 5 or 10 μM
Incubation time 48 hours
Animal Experiment
Animal models
Formulation
Dosages
Administration
Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.

Chemical Information
Molecular Weight 246.31
Formula C17H14N2
CAS Number 519-23-3
Purity >98%
Solubility DMSO 10 mM
Storage at -20°C
References

[1] Stiborova M, et al. Neuro Endocrinol Lett. The effect of benzo[a]pyrene on metabolic activation of anticancer drug ellipticine in mice.

[2] Pandrangi SL, et al. Tumour Biol. Effects of ellipticine on ALDH1A1-expressing breast cancer stem cells--an in vitro and in silico study.

[3] Stiborova M, et al. Interdiscip Toxicol. Ellipticine cytotoxicity to cancer cell lines - a comparative study.

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  Catalog
Abmole Inhibitor Catalog 2017




Keywords: Ellipticine, CCG36483; NSC71795 supplier, Topoisomerase, inhibitors

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