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AS-1413 (Amonafide) | DNA intercalator

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Price:
$109.00
Catalog #:
C2714-5
Quantity:


Product Description

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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