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Ellipticine hydrochloride

Catalog No. T4614 CAS 5081-48-1

Synonyms: Ellipticine HCl, NSC 71795 (hydrochloride)

Ellipticine hydrochloride (NSC-71795 (hydrochloride)) is a potent antineoplastic agent; inhibits DNA topoisomerase II activities.

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Ellipticine hydrochloride Chemical Structure

Ellipticine hydrochloride, CAS 5081-48-1

Pack Size	Availability	Price/USD
5 mg	In stock	$ 50.00
10 mg	In stock	$ 73.00
25 mg	In stock	$ 148.00
50 mg	In stock	$ 262.00
100 mg	In stock	$ 388.00
1 mL * 10 mM (in DMSO)	In stock	$ 50.00

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Purity: 98.85%

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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] .

Synonyms	Ellipticine HCl, NSC 71795 (hydrochloride)
Molecular Weight	282.76
Formula	C17H15ClN2
CAS No.	5081-48-1

Storage

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

Solubility Information

DMSO: 5.8 mg/mL (20.51 mM), Sonication and heating are recommended.

References and Literature

1. Stiborova M, et al. Molecular mechanisms of antineoplastic action of an anticancer drug ellipticine. Biomed Pap Med Fac Univ Palacky Olomouc Czech Repub. 2006 Jul;150(1):13-23. 2. Stiborova M, et al. Ellipticine cytotoxicity to cancer cell lines - a comparative study. Interdiscip Toxicol. 2011 Jun;4(2):98-105. 3. Stiborova M, et al. The anticancer drug ellipticine activated with cytochrome P450 mediates DNA damage determining its pharmacological efficiencies: studies with rats, Hepatic Cytochrome P450 Reductase Null (HRN™) mice and pure enzymes. Int J Mol Sci. 2014 Dec 25;16(1):284-306. 5. Wang W, Shu M, Nie A, et al. Ultrasensitive evaluation of Ribonuclease H activity using a DNAzyme-powered on-particle DNA walker[J]. Sensors and Actuators B: Chemical. 2020, 304: 127380.

Citations

1. Wang W, Shu M, Nie A, et al. Ultrasensitive evaluation of Ribonuclease H activity using a DNAzyme-powered on-particle DNA walker. Sensors and Actuators B: Chemical. 2020, 304: 127380 2. Li X, Ye C, Mulati M, et al. Ellipticine blocks synergistic effects of IL-17A and TNF-α in epithelial cells and alleviates severe acute pancreatitis-associated acute lung injury. Biochemical Pharmacology. 2020: 113992.

Related compound libraries

This product is contained In the following compound libraries：

Inhibitor Library Anti-Cancer Active Compound Library Anti-Aging Compound Library Bioactive Compound Library Natural Product Library Anti-Tumor Natural Product Library Bioactive Compounds Library Max DNA Damage & Repair Compound Library Selected Plant-Sourced Compound Library Alkaloid Natural Product Library

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Keywords

Ellipticine hydrochloride 5081-48-1 DNA Damage/DNA Repair Topoisomerase Inhibitor Ellipticine HCl NSC71795 NSC 71795 (hydrochloride) Ellipticine NSC-71795 Ellipticine Hydrochloride NSC 71795 inhibit inhibitor

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