1H-Benz[de]isoquinoline-1,3(2H)-dione, 5-amino-2-[2-(dimethylamino)ethyl]-
Amonafide
CAS: 69408-81-7
Molecular Formula: C16H17N3O2
1H-Benz[de]isoquinoline-1,3(2H)-dione, 5-amino-2-[2-(dimethylamino)ethyl]- - Names and Identifiers
1H-Benz[de]isoquinoline-1,3(2H)-dione, 5-amino-2-[2-(dimethylamino)ethyl]- - Physico-chemical Properties
| Molecular Formula | C16H17N3O2 |
| Molar Mass | 283.33 |
| Density | 1.306±0.06 g/cm3(Predicted) |
| Melting Point | 162-164°C |
| Boling Point | 500.2±35.0 °C(Predicted) |
| Solubility | DMSO (Slightly), Methanol (Slightly) |
| Appearance | Solid |
| Color | Yellow to Dark Yellow |
| pKa | 8.83±0.28(Predicted) |
| Storage Condition | Keep in dark place,Sealed in dry,2-8°C |
| In vitro study | Amonafide treatment results in DNA single-strand breaks (SSB), double-strand breaks (DSB), and DNA protein cross-linking in human myeloid leukemia cells via a topoisomerase II-mediated response. Amonafide treatment dose-dependently inhibits colony formation in leukemic cell lines and normal human bone marrow GM-CFC. Amonafide did not cause topoisomerase I-mediated DNA fragmentation even at 100 μm concentrations. m-AMSA resistant cell lines were less than 2-fold resistant to Amonafide. Amonafide interferes with the DNA break-repolymerization activity of mammalian DNA topoisomerase II, resulting in activation of DNA breaks. The distribution of breaking strength stimulated by Amonafide was significantly different compared to other antineoplastic agents. Aside from guanine and thymine, Amonafide has a high affinity for cytosine at site -1 and a lower affinity for adenine at site -1. Amonafide-induced topoisomerase II-mediated DNA fragmentation was only slightly affected (less than 3-fold) by 1 mM ATP, indicating that compared with doxorubicin,etoposide, and mitoxantrone, amonafide is an ATP-insensitive topoisomerase II inhibitor. Amonafide significantly inhibited the growth of HT-29,HeLa, and PC3 cells with IC50 of 4.67 μm, 2.73 μm, and 6.38 μm, respectively. Unlike those classical topoisomerase II inhibitors (daunorubicin,doxorubicin,idarubicin,etoposide, and mitoxantrone),Amonafide is not affected by P-glycoprotein-mediated efflux. |
1H-Benz[de]isoquinoline-1,3(2H)-dione, 5-amino-2-[2-(dimethylamino)ethyl]- - Preparation solution concentration reference
| 1mg | 5mg | 10mg | |
|---|---|---|---|
| 1 mM | 3.529 ml | 17.647 ml | 35.295 ml |
| 5 mM | 0.706 ml | 3.529 ml | 7.059 ml |
| 10 mM | 0.353 ml | 1.765 ml | 3.529 ml |
| 5 mM | 0.071 ml | 0.353 ml | 0.706 ml |
Last Update：2024-01-02 23:10:35
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