Amonafide is a DNA intercalating agent and inhibitor of topoisomerase II that has been extensively studied in patients with malignant solid tumors. Topoisomerase II-mediated DNA cleavage induced by Amonafide is affected only slightly (less than 3-fold) by 1 mM ATP, suggeting that Amonafide is an ATP-insensitive topoisomerase II inhibitor in contrast to doxorubicin, etoposide, and mitoxantrone. Amonafide significantly inhibits the growth of HT-29, HeLa, and PC3 cells with IC50 of 4.67 μM, 2.73 μM, and 6.38 μM, respectively. Amonafide (originally AS1413) is a new imide derivative of naphthalic acid. It belongs to the families of drugs called topoisomerase inhibitors and DNA intercalators. Amonafide (trade name Quinamed) has shown significant efficacy for remission induction in patients with sAML in combination with cytarabine. Amonafide is a promising therapeutic candidate directed toward bypassing this common mechanism of compound resistance encountered in the treatment of patients with AML, and possibly in other resistant hematological malignancies as well.
|Body Surface Area (m2)||0.007||0.025||0.15||0.05||0.02||0.5|
|Animal A (mg/kg) = Animal B (mg/kg) multiplied by||Animal B Km|
|Animal A Km|
For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 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 resveratrol of 11.2 mg/kg.
|Solubility||DMSO 50 mg/mL|
Amonafide, a topoisomerase II inhibitor, is unaffected by P-glycoprotein-mediated efflux.
Chau M, et al. Leuk Res. 2008 Mar;32(3):465-73. PMID: 17826829.
Amonafide: An active agent in the treatment of previously untreated advanced breast cancer--a cancer and leukemia group B study (CALGB 8642).
Costanza ME, et al. Clin Cancer Res. 1995 Jul;1(7):699-704. PMID: 9816035.
|Related Topoisomerase Products|
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Pixantrone dimaleate is a topoisomerase II inhibitor and DNA intercalator, with anti-tumor activity.
10-Hydroxycamptothecin is a cell-permeable powerful DNA topoisomerase I inhibitor. It has selective inhibitory effect on the phosphorylation of histone H1 and H3, but less effect on other histones.
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