Pyrazoloacridine (NSC 366140), an intercalating agent with anti-cancer activity, inhibits the activity of topoisomerases 1 and 2. Pyrazoloacridine (NSC 366140) exhibits an IC50 of 1.25 μM in K562 myeloid leukemia cells for 24 h treatment[1][2].
Pyrazoloacridine (NSC 366140, PD 115934) exhibits IC50 values of 10.7 μM and 4.5 μM for oxic and hypoxic HCT-8 cells[1].Pyrazoloacridine (NSC 366140, 2-4 μM) abolishes the catalytic activity of both topo I and topo II in vitro[2].Pyrazoloacridine (NSC 366140) displays activity against cisplatin- and paclitaxel-resistant ovarian cancer[2].Pyrazoloacridine (NSC 366140) has been shown to cause delayed DNA fragmentation in MCF-7 breast cancer cells[2].Pyrazoloacridine (NSC 366140) induces apoptosis in P53-deficient Hep 3B human hepatoma cells[2]. Cell Cytotoxicity Assay[2] Cell Line: K562 Myeloid Leukemia Cells.
[1]. J S Sebolt, et al. Pyrazoloacridines, a new class of anticancer agents with selectivity against solid tumors in vitro. Cancer Res. 1987 Aug 15;47(16):4299-304. [2]. A A Adjei, et al. Effect of pyrazoloacridine (NSC 366140) on DNA topoisomerases I and II. Clin Cancer Res. 1998 Mar;4(3):683-91.