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Ellipticine hydrochloride

Cat. No. M9695
Ellipticine hydrochloride Structure
Synonym:

NSC71795 hydrochloride

Size Price Availability Quantity
5mg USD 60  USD60 In stock
10mg USD 90  USD90 In stock
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Quality Control & Documentation
Biological Activity

Ellipticine (NSC71795) hydrochloride is a potent antineoplastic agent which inhibits DNA topoisomerase II activities. The mechanisms of Ellipticine (NSC71795) antitumor, mutagenic and cytotoxic activities are suggested to be intercalation into DNA and inhibition of DNA topoisomerase II activity. Another mode of Ellipticine (NSC71795) action is the formation of covalent DNA adducts mediated by its oxidation with cytochromes P450 (CYP) and peroxidases. The induced expression of cytochrome b5 protein in liver of rats treated with Ellipticine (NSC71795) suggests that cytochrome b5 may modulate the CYP-mediated bioactivation and detoxification of Ellipticine (NSC71795).

Chemical Information
Molecular Weight 282.77
Formula C17H15ClN2
CAS Number 5081-48-1
Solubility (25°C) DMSO 10 mM
Storage Powder          -20°C   3 years ;  4°C   2 years
In solvent       -80°C   6 months ;  -20°C   1 month
Conversion of different model animals based on BSA (PMID: 27057123)
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.

References

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

[2] Marie Stiborova, et al. Biomed Pap Med Fac Univ Palacky Olomouc Czech Repub. Molecular mechanisms of antineoplastic action of an anticancer d rvg ellipticine

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Keywords: Ellipticine hydrochloride, NSC71795 hydrochloride supplier, Topoisomerase, inhibitors, activators


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