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Amonafide

CAS No. : 69408-81-7

MCE 国际站：Amonafide

产品活性：Amonafide 是一种拓扑异构酶 II (topoisomerase II) 的抑制剂和 DNA 的嵌入剂，通过抑制 Topo II 与 DNA 的结合，来诱导凋亡信号通路的发生。

研究领域：Cell Cycle/DNA Damage

作用靶点：Topoisomerase

In Vitro: Amonafide is a topoisomerase II inhibitor and DNA intercalator that induces apoptotic signaling by blocking the binding of Topo II to DNA. Amonafide produces protein-associated DNA cleavage, single-strand breaks (SSB) and DPC and DNA double-strand cleavage. Amonafide (Nafidimide, 400 nM-2.4 μM) reduces the colony-forming ability of the leukemic cell lines in a dose-dependent manner. Amonafide (0.05-0.4 μg/mL) reduces several tumor growth. However, Amonafide is active against only 12% of tumors compared with standard agents (5-fluorouracil, mitomycin C, cisplatin, and etoposide), which are active against more than 40% of tumors in the human bone marrow inhibitory range. Amonafide inhibits the growth of HT-29, HeLa, and PC-3 cell lines, with IC₅₀s of 4.67, 2.73, and 6.38 μM.

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