- 生物活性
Pyrazoloacridine (NSC 366140) 具有抗癌活性，抑制拓扑异构酶 1 和 2 的活性 (topoisomerases 1 and 2)。Pyrazoloacridine (NSC 366140) 对 K562 髓系白血病细胞中的 IC50 值为 1.25 μM (24 h)。
- 体外研究
Pyrazoloacridine (NSC 366140, PD 115934) exhibits IC
50
values of 10.7 μM and 4.5 μM for oxic and hypoxic HCT-8 cells.
Pyrazoloacridine (NSC 366140, 2-4 μM) abolishes the catalytic activity of both topo I and topo II in vitro.
Pyrazoloacridine (NSC 366140) displays activity against cisplatin- and paclitaxel-resistant ovarian cancer.
Pyrazoloacridine (NSC 366140) has been shown to cause delayed DNA fragmentation in MCF-7 breast cancer cells.
Pyrazoloacridine (NSC 366140) induces
apoptosis
in P53-deficient Hep 3B human hepatoma cells.
Cell Cytotoxicity Assay
Cell Line:
K562 Myeloid Leukemia Cells.
Concentration:
0-500 μM.
Incubation Time:
1 h or 24 h.
Result:
When K562 cells were incubated with PA for 1 h and then plated in soft agar, an IC
50
of -50 μM was observed. In contrast, when cells were incubated for 24 h with PA, the IC
50
was 1.25 μM.
