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10mM in DMSO for sensitive chromatographic and analytical workflows requiring minimal baseline interference.
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Cited in 0 peer-reviewed publications across chromatography, organic synthesis, and cross-coupling reactions.
Information
Amonafide (NSC308847, AS1413) produces protein-associated DNA-strand breaks through atopoisomerase II-mediated reaction, but does not produce topoisomerase I-mediated DNA cleavage. Phase 3.
In vitro
Through a topoisomerase II-mediated reaction, Amonafide treatment produces DNA single-strand breaks (SSB), double-strand breaks (DSB), and DNA-protein cross-links in human myeloid leukemia cells. Amonafide treatment inhibits conlony formation of the leukemic cell lines and the normal human bone marrow GM-CFC in a dose-dependent manner. Amonafide does not produce topoisomerase I-mediated DNA cleavage even at 100 μM. The m-AMSA-resistant line is less than 2-fold resistant to Amonafide Amonafide interferes with the DNA breakage-reunion activity of mammalian DNA topoisomerase II resulting in DNA cleavage stimulation. Compared with those of other antitumor drugs, Amonafide-stimulated cleavage intensity patterns are markedly different. Amonafide highly prefers a cytosine, and excludes guanines and thymines instead, at position -1, with lower preference for an adenine at position +1. 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 is unaffected by P-glycoprotein-mediated efflux, unlike those of the classical topoisomerase II inhibitors (daunorubicin, doxorubicin, idarubicin, etoposide, and mitoxantrone).
In vivo
Cell Data
cell lines:HMC-1, IC-2, CBhCMCs cells
Concentrations:Dissolved in DMSO, final concentrations ~10 μM
Incubation Time:72 hours
Powder Purity:≥99%
| Isomeric SMILES | CN(C)CCN1C(=O)C2=CC=CC3=CC(=CC(=C32)C1=O)N |
|---|---|
| Molecular Weight | 283.33 |
| Reaxy-Rn | 5344673 |
| Reaxys-RN_link_address | https://www.reaxys.com/reaxys/secured/hopinto.do?context=S&query=IDE.XRN=5344673&ln= |
Comprehensive hazard, handling, storage, and regulatory compliance document.
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View spec sheet →| Solubility | Solubility (25°C) In vitro DMSO: 46 mg/mL (198.07 mM); Ethanol: 46 mg/mL (198.07 mM); Water: Insoluble; |
|---|---|
| Melt Point(°C) | 162-164°C |