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米托蒽醌二盐酸盐, DNA 拓扑异构酶 II alpha 抑制剂

II型拓扑异构酶抑制剂
    级别和纯度:
  • 10mM in DMSO
  • CAS编号: 70476-82-3
  • 分子式: C22H28N4O6·2HCl
  • 分子量: 517.4
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库存信息

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货号 (SKU) 包装规格 是否现货 价格 数量
M408662-1ml
1ml 现货 Stock Image
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Compound libraries (12333)

基本描述

英文别名 1,4-dihydroxy-5,8-bis(2-(2-hydroxyethylamino)ethylamino)anthracene-9,10-dione dihydrochloride
规格或纯度 10mM in DMSO
英文名称 Mitoxantrone (NSC-301739) 2HCl
生化机理 Mitoxantrone 2HCl (NSC-301739) 是 Mitoxantrone 的二盐酸盐。米托蒽醌是 II 型拓扑异构酶和蛋白激酶 C (PKC) 的抑制剂,对 PKC 的 IC50 值为 8.5 μM。米托蒽醌可抑制 MCF-7/wt 细胞的增殖生长,IC50 为 0.42 μM。米托蒽醌还能诱导细胞凋亡。
储存温度 -80℃储存
运输条件 超低温冰袋运输
作用类型 抑制剂
作用机制 DNA 拓扑异构酶 II alpha 抑制剂
产品介绍


Information

Mitoxantrone 2HCl (NSC-301739) is a dihydrochloride salt of Mitoxantrone. Mitoxantrone is an inhibitor oftype II topoisomeraseandprotein kinase C (PKC)with IC50 of 8.5 μM for PKC. Mitoxantrone inhibits cell proliferative growth of MCF-7/wt cells with IC50
In vitro

Mitoxantrone induces DNA fragmentation and the proteolytic cleavage of poly(ADP-ribose) polymerase (PARP), a marker of the activation of caspases, in all the patients studied, demonstrating that the cytotoxic effect of mitoxantrone is due to induction of apoptosis. Mitoxantrone activates NFkappaB and stimulates IkappaBalpha degradation in the promyelocytic leukemia cell line HL60 but not in the variant cells, HL60/MX2 cells, which lack the beta isoform of topoisomerase II and express a truncated alpha isoform that results in an altered subcellular distribution. Mitoxantrone inhibits proliferation of activated PBMCs, B lymphocytes, or antigen-specific T-cell lines (TCLs) stimulated on antigen-presenting cells (APCs) in a dose-dependent manner. Mitoxantrone induces apoptosis of PBMCs, monocytes and DCs at low concentrations, whereas higher doses causes cell lysis.

In vivo

Mitoxantrone transiently decreases the growth rate of HID xenografts in mice but does not affect that of PAC120 xenografts. Mitoxantrone results in the severity of the cardiac lesions and the nephropathy and the intestinal toxicity in spontaneously hypertensive rats. Mitoxantrone and iron(III) form a strong 2:1 complex, in which mitoxantrone may be acting as a tridentate ligand.
Cell Data

cell lines:

Concentrations:

Incubation Time:

Powder Purity:≥95%

名称和识别符

Isomeric SMILES C1=CC(=C2C(=C1NCCNCCO)C(=O)C3=C(C=CC(=C3C2=O)O)O)NCCNCCO.Cl.Cl
关联CAS 65271-80-9
PubChem CID 51082
分子量 517.4

化学和物理性质

溶解性 Solubility (25°C) In vitro DMSO: 4.89 mg/mL (37.85 mM);    
熔点 267 °C(dec.)

安全和危险性(GHS)

象形图 GHS08
信号词 Danger
危险声明

H360: 可能损害生育力或未出生的孩子

H340: 可能导致遗传缺陷

预防措施声明

P280: 戴防护手套/穿防护服/戴防护眼罩/戴防护面具。

P405: 密闭存放

P501: 将内容物/容器处理到。。。

P281: 根据需要使用个人防护设备。

P203: 使用前,获取、阅读并遵守所有安全说明。

P318: 如果暴露或担心,请就医。

Merck Index 6217

质检证书(CoA,COO,BSE/TSE 和分析图谱)

C of A & Other Certificates(BSE/TSE, COO):
输入批号以搜索分析图谱:

技术文档和文章

溶液计算器