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Ellipticine hydrochloride

Ellipticine hydrochloride
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Purity:98.85%
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Ellipticine hydrochloride

Catalog No. T4614Cas No. 5081-48-1
Ellipticine hydrochloride (NSC-71795 (hydrochloride)) is a potent antineoplastic agent; inhibits DNA topoisomerase II activities.
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Pack SizePriceAvailabilityQuantity
5 mg$40In Stock
10 mg$60In Stock
25 mg$123In Stock
50 mg$213In Stock
100 mg$313In Stock
1 mL x 10 mM (in DMSO)$44In Stock
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Product Introduction

Bioactivity
Description
Ellipticine hydrochloride (NSC-71795 (hydrochloride)) is a potent antineoplastic agent; inhibits DNA topoisomerase II activities.
In vitro
Ellipticine is a potent antineoplastic agent exhibiting the multimodal mechanism of its action. The mechanisms of ellipticine antitumor, mutagenic and cytotoxic activities are suggested to be intercalation into DNA and inhibition of DNA topoisomerase II activity. Another mode of ellipticine action is the formation of covalent DNA adducts mediated by its oxidation with cytochromes P450 (CYP) and peroxidases[1]. Ellipticine can also 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. This effect is associated with formation of two covalent ellipticine-derived DNA adducts[2].
In vivo
Ellipticine treatment results in ellipticine-derived DNA adduct generation in several healthy organs (liver, kidney, lung, spleen, breast, heart and brain) and in DNA of mammary adenocarcinoma. The levels of ellipticine-derived DNA adducts generated in these adenocarcinomas are almost 2-fold higher than in normal healthy mammary tissue. 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[3].
Cell Research
The cytotoxicity of ellipticine is determined by MTT test. Ellipticine is dissolved in DMSO (1 mM) and diluted in culture medium to final concentrations of 0, 0.1, 1, 5 or 10 μM. Cells in exponential growth are seeded at 1×104 per well in a 96-well microplate. After incubation the MTT solution is added, the microplates are 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 is measured. The mean absorbance of medium controls is subtracted as a background. The viability of control cells is taken as 100% and the values of treated cells are calculated as a percentage of control. The IC50 values are calculated using linear regression of the dose-log response curves[2] .
AliasEllipticine HCl, NSC 71795 (hydrochloride)
Chemical Properties
Molecular Weight282.76
FormulaC17H15ClN2
Cas No.5081-48-1
Storage & Solubility Information
StoragePowder: -20°C for 3 years | In solvent: -80°C for 1 year
Solubility Information
DMSO: 5.8 mg/mL (20.51 mM)
Solution Preparation Table
DMSO
1mg5mg10mg50mg
1 mM3.5366 mL17.6828 mL35.3657 mL176.8284 mL
5 mM0.7073 mL3.5366 mL7.0731 mL35.3657 mL
10 mM0.3537 mL1.7683 mL3.5366 mL17.6828 mL
20 mM0.1768 mL0.8841 mL1.7683 mL8.8414 mL

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