A DNA-intercalating topoisomerase II poison; reduces the formation of kinetoplast DNA minicircles in a cell-free assay at 100 µM

Amonafide – 100 mg

Brand:
Cayman
CAS:
69408-81-7
Storage:
-20
UN-No:
Non-Hazardous - /

Amonafide is a DNA-intercalating topoisomerase II poison.{59203} It reduces the formation of kinetoplast DNA minicircles, a marker of topoisomerase II activity, in a cell-free assay at 100 µM, but does not induce relaxation of supercoiled DNA, a marker of topoisomerase I activity, at the same concentration.{59204} Amonafide inhibits growth in a panel of 11 human cancer cell lines, including leukemia, gastric, breast, and lung cancer cells, with GI50 values ranging from 1 to 10 µM.{59205} It induces cell cycle arrest at the G2/M phase and apoptosis in AGS gastric and Huh7 hepatoma cancer cells, respectively, when used at concentrations ranging from 2.5 to 10 µM. Amonafide (5 mg/kg) reduces primary tumor growth and decreases pulmonary metastasis in a murine H22 hepatoma model.{59206}  

 

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SKU: 31623 - 100 mg Category:

Description

A DNA-intercalating topoisomerase II poison; reduces the formation of kinetoplast DNA minicircles in a cell-free assay at 100 µM, but does not induce relaxation of supercoiled DNA; inhibits growth in a panel of 11 human cancer cell lines including leukemia, gastric, breast, and lung cancer cells (GI50s = 1-10 µM); induces cell cycle arrest at the G2/M phase and apoptosis in AGS gastric and Huh7 hepatoma cancer cells, respectively, from 2.5-10 µM; reduces primary tumor growth and decreases pulmonary metastasis in a murine H22 hepatoma model at 5 mg/kg

Formal name: 5-amino-2-[2-(dimethylamino)ethyl]-1H-benz[de]isoquinoline-1,3(2H)-dione

Synonyms:  AS1413|Benzisoquinolinedione|Nafidimide|NCI 308847|NSC 308847

Molecular weight: 283.3

CAS: 69408-81-7

Purity: ≥98%

Formulation: A crystalline solid

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