Pyrazoloacridine(Synonyms: NSC 366140; PD 115934)

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Pyrazoloacridine (Synonyms: NSC 366140; PD 115934) 纯度: ≥98.0%

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)。

Pyrazoloacridine(Synonyms: NSC 366140; PD 115934)

Pyrazoloacridine Chemical Structure

CAS No. : 99009-20-8

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Pyrazoloacridine 相关产品

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生物活性

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].

体外研究
(In Vitro)

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].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Cytotoxicity Assay[2]

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 IC50 of -50 μM was observed. In contrast, when cells were incubated for 24 h with PA, the IC50 was 1.25 μM.

Clinical Trial

分子量

367.40

Formula

C19H21N5O3
CAS 号

99009-20-8
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
溶解性数据
In Vitro: 

DMSO : < 1 mg/mL (ultrasonic) (insoluble or slightly soluble)
参考文献

  • [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.

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