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抑制剂/激动剂
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/ 拓扑异构酶 / Bisantrene

比生群 /Bisantrene {[allProObj[0].p_purity_real_show]}

货号：A518842 同义名： CL216942;CS1

Bisantrene是一种抗癌剂，通过影响 DNA 插入发挥细胞毒性，靶向真核生物的拓扑异构酶 II。

Bisantrene 化学结构 CAS号：78186-34-2
Bisantrene 化学结构
CAS号：78186-34-2
Bisantrene 3D分子结构
CAS号：78186-34-2
Bisantrene 化学结构 CAS号：78186-34-2
Bisantrene 3D分子结构 CAS号：78186-34-2
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Bisantrene 纯度/质量文件 产品仅供科研

货号：A518842 标准纯度： {[allProObj[0].p_purity_real_show]}
批次查询： 批次纯度:

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产品名称 Topo I ↓ Topo II ↓ Topo IV ↓ Topoisomerase ↓ 其他靶点 纯度
Ellagic acid ✔ 98%
β-Lapachone ✔ 99%+
(s)-10-hydroxycamptothecin ✔ 98+%
Camptothecin ++

Topo I, IC50: 0.68 μM

 		98%
Betulinic acid ++

Eukaryotic topoisomerase I, IC50: 5 μM

 		98%
Topotecan ++++

Topo I (MCF-7 Luc cells), IC50: 13 nM

Topo I (DU-145 Luc cells), IC50: 2 nM

 		98%
Irinotecan HCl Trihydrate ✔ 98%
SN-38 ✔ 98%
Levofloxacin hydrate ✔ 98%
Dexrazoxane ✔ 99%+
Ofloxacin ✔ 98+%
Enoxacin ✔ 99%+
Flumequine +

Topo II, IC50: 15 μM

 		98%
Levofloxacin ✔ 97%
Etoposide ✔ 98%
Pefloxacin mesylate dihydrate ✔ 99+%
Marbofloxacin ✔ 98+%
Voreloxin HCl ✔ 98%
Mitoxantrone dihydrochloride ✔ PKC 98%
Nalidixic acid ✔ 98%
Doxorubicin ✔ 98%
Novobiocin sodium ✔ 95%
Amonafide ✔ 99%+
Pirarubicin ✔ 98%+
Idarubicin HCl +++

Topo II (MCF-7 cells), IC50: 3.3 ng/mL

 		99%+
Genistein ✔ EGFR 98%
Teniposide ✔ 98%
Moxifloxacin ✔ 98%
Ciprofloxacin ✔ 98%
Clinafloxacin ✔ 99%
Gatifloxacin ✔ 98%
Daunorubicin HCl +++

DNA synthesis, Ki: 20 nM

 		98%
Epirubicin HCl ✔ 99%+
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多，抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用，但抑制强度暂时没有相关数据。

Bisantrene 生物活性

描述 Bisantrene, recognized for its potent antitumor properties, achieves its cytotoxic effects through DNA intercalation. It specifically interacts with eukaryotic type II topoisomerases and is also identified as a substrate for MDR1[1][2][3][4]. Bisantrene enhances DNase I cleavage at oligopurine-oligopyrimidine sequences and marginally diminishes the cleavage at alternating purine-pyrimidine sequences[1]. Bisantrene acts as an inhibitor of [3H]uridine integration into RNA and [3H]thymidine integration into DNA[2].

Bisantrene 动物研究

Animal study Bisantrene's efficacy spans a dosage range from 1.56 to 150 mg/kg, varying according to the treatment's frequency, administration method, and schedule, as well as the tumor model utilized. Pre-treatment with Bisantrene at doses of 25, 50, and 100 mg/kg, administered intraperitoneally once, in conjunction with macrophages, demonstrates an antitumor effect in mice injected with P815 tumor cells[3]. Administered intravenously in a single dose ranging from 10 to 150 mg/kg, Bisantrene causes leukopenia in Neo mice in a dose-dependent manner. Both B cells and macrophages are susceptible to the toxic effects of Bisantrene[4].

Bisantrene 参考文献

[1]Sissi C, et al. DNA-binding preferences of Bisantrene analogues: relevance to the sequence specificity of drug-mediated topoisomerase II poisoning. Mol Pharmacol. 1998 Dec;54(6):1036-45.

[2]Yap HY, et al. Bisantrene, an active new drug in the treatment of metastatic breast cancer. Cancer Res. 1983 Mar;43(3):1402-4.

[3]Wang BS, et al. Activation of tumor-cytostatic macrophages with the antitumor agent 9,10-anthracenedicarboxaldehyde bis[(4,5-dihydro-1H-imidazole-2-yl)hydrazone] dihydrochloride (bisantrene). Cancer Res. 1984 Jun;44(6):2363-7.

[4]Aksentijevich I, et al. Retroviral transfer of the human MDR1 gene confers resistance to bisantrene-specific hematotoxicity. Clin Cancer Res. 1996 Jun;2(6):973-80.

Bisantrene 实验方案

计算器
存储液制备 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.51mL

0.50mL

0.25mL

12.55mL

2.51mL

1.25mL

25.10mL

5.02mL

2.51mL

Bisantrene 技术信息

CAS号78186-34-2
分子式C22H22N8
分子量 398.464
别名 CL216942;CS1
运输蓝冰
存储条件

In solvent -20°C:3-6个月-80°C:12个月

Pure form Sealed in dry,Room Temperature
溶解度

DMSO: 1 mg/mL(2.51 mM)，配合低频超声，并水浴加热至45℃助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
动物实验配方

Tags: Bisantrene | 78186-34-2 | CL216942 | CL 216942 | CL-216942 | Cell Cycle/DNA Damage | Topoisomerase | 仅供科研使用 | AmBeed-信号通路专用抑制剂 | Bisantrene 纯度/质量文件 | Bisantrene 亚型比较 | Bisantrene 生物活性 | Bisantrene 参考文献 | Bisantrene 实验方案 | Bisantrene 技术信息

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