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).
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 |
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.
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