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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.
| Molecular Weight | 283.33 |
| Formula | C16H17N3O2 |
| CAS Number | 69408-81-7 |
| Solubility (25°C) | DMSO 47 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| Related Topoisomerase Products |
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| Camptothecin
Camptothecin (CPT), an alkaloid, is an inhibitor of DNA Topoisomerase I (Topo I) with an IC50 value of 679 nM. Camptothecin (CPT) has strong antitumor activity against colorectal cancer, breast cancer, lung cancer and ovarian cancer, and modulates hypoxia-inducible factor-1α (HIF-1α) activity by altering miRNA expression patterns in human cancer cells. |
| Ellagic acid
Ellagic acid is a natural antioxidant as well as a potent, ATP-competitive inhibitor of CK2 and SHP2 with IC50 and Ki values of 40 nM and 20 nM, respectively.In addition, Ellagic acid exhibits antiproliferative activity and inhibition of topoisomerase II (Topoisomerase II). |
| Pirarubicin
Pirarubicin is an anthracycline that is an inhibitor of Topoisomerase II.*The compound is unstable in solutions, freshly prepared is recommended |
| β-Lapachone
β-Lapachone is a selective DNA topoisomerase I inhibitor, exhibiting no inhibitory activities against DNA topoisomerase II or ligase. |
| Flumequine
Flumequine is a synthetic chemotherapeutic antibiotic, inhibiting topoisomerase II with IC50 of 15 μM. |
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