Pixantrone (topoisomerase II抑制剂)

化学名

6,9-bis(2-aminoethylamino)benzo[g]isoquinoline-5,10-dione

简称

Pixantrone

别名

Pixuvri, BBR-2778, BBR2778, BBR 2778

中文名

匹杉琼

化学式

C₁₇H₁₉N₅O₂

分子量

325.37

CAS号

144510-96-3

纯度

98%

溶剂/溶解度

Water<1mg/ml; DMSO4mg/ml; Ethanol<1mg/ml

溶液配制

5mg加入1.54ml DMSO，或者每3.25mg加入1ml DMSO，配制成10mM溶液。SF1168-10mM用DMSO配制。

产品描述

Pixantrone (BBR 2778) is an experimental antineoplastic drug.

信号通路

Others

靶点

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IC50

－

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体外研究

Pixantrone is an experimental antineoplastic (anti-cancer) drug, an analogue of mitoxantrone with fewer toxic effects on cardiac tissue, It acts as a topoisomerase II poison and intercalating agent. Pixantrone may be useful in patients pretreated with anthracyclines. An in vitro crosslinking assay demonstrated that Pixantrone is efficiently activated by formaldehyde to generate covalent drug-DNA adducts capable of stabilizing double-stranded DNA in denaturing conditions. Pixantrone-DNA adduct formation is both concentration and time dependent and the reaction exhibits an absolute requirement for formaldehyde. Pixantrone exhibited a 10- to 100-fold greater propensity to generate adducts at equimolar formaldehyde and drug concentrations. Pixantrone-DNA adducts are thermally and temporally labile, yet they exhibit a greater thermal midpoint temperature and an extended half-life at 37 degrees C when compared to mitoxantrone-DNA adducts.

体内研究

N/A

临床实验

N/A

特征

N/A

酶活性检测实验

方法

N/A

细胞实验

细胞系

N/A

浓度

N/A

处理时间

N/A

方法

N/A

动物实验

动物模型

N/A

配制

N/A

剂量

N/A

给药方式

N/A

产品编号

产品名称

包装

KL1168-10mM

Pixantrone (topoisomerase II抑制剂)

10mM×0.2ml

KL1168-5mg

Pixantrone (topoisomerase II抑制剂)

5mg

KL1168-25mg

Pixantrone (topoisomerase II抑制剂)

25mg

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说明书

1份