Amonafide (AS-1413) is a reversible, benzoisoquinolinedione-based DNA intercalator that produces protein-associated DNA cleaveage and single- and double-strand cleavage by mechanisms suggesting an interaction with topoisomerase II. [1]Amonafide has demonstrated significant activity against P388 leukemia and L1210 cell lines as well as B16 melanoma and M5076 sarcoma cell lines. [2] In phase II studies with cytarabine, overall CR rates of 42% were observed and produced a high complete remission rate and durable responses in patients with acute myeloid leukemia. [3]Amonafide is easily metabolized and is a substrate of N-acetyl transferase-2 (NAT2); the acetylation adduct is roughly equipotent to amonafide, but has been attributed to the toxicity observed in the clinic. [4]
Technical information:
| Chemical Formula: | C16H17N3O2 | |
| CAS #: | 69408-81-7 | |
| Molecular Weight: | 283.33 | |
| Purity: | >98% | |
| Appearance: | Yellow | |
| Chemical Name: | 1H-Benz[de]isoquinoline-1,3(2H)-dione, 5-amino-2-[2-(dimethylamino)ethyl]- | |
| Solubility: | Up to 100 mM in DMSO | |
| Synonyms: | AS-1413, AS1413, Amonafide, Nafidimide, 5-Aminomitonafide, NSC308847 |
Shipping Condition: The product is shipped in a glass vial at ambient temperature.Storage condition: For longer shelf life, store solid powder at 4oC desiccated, or store DMSO solution at -20oC.
Reference:
| 1. | Andersson et al., In vitro toxicity and DNA cleaving capacity of benzisoquinolinedione (nafidimide; NSC 308847) in human leukemia. Cancer Res. 1987, 47, 1040-1044. Pubmed ID:3026621 |
| 2. | Costanza et al., Amonafide: An active agent in the treatment of previously untreated advanced breast cancer--a cancer and leukemia group B study (CALGB 8642). Clin Cancer Res., 1995, 1, 699-704. Pubmed ID:9816035 |
| 3. | Zhu et al., Novel agents and regimens for acute myeloid leukemia: 2009 ASH annual meeting highlights. J. Hemat. Oncol. 2010, 3, 17-26. Pubmed ID:20416083 |
| 4. | Innocenti et al., Pharmacogenetics of anticancer agents: lessons from amonafide and irinotecan. Drug Met. Dispos. 2001, 29(4), 596-600. Pubmed ID:9816035 |
Other Information:
Product Specification (pdf) MSDS (pdf) Certificate of Analysis is available upon request.
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