化学信息:
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。
|
生物信息:
产品描述
|
Pixantrone (BBR 2778) is an experimental antineoplastic drug.
|
信号通路
|
Others
|
靶点
|
-
|
-
|
-
|
-
|
-
|
IC50
|
-
|
-
|
-
|
-
|
-
|
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
|
相关实验数据(此数据来自于公开文献,碧云天并不保证其有效性):
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
|
参考文献:
1. Cavalletti, E., et al.Invest New Drugs, 2007. 25(3), 187-95.
2. Evison, B.J., et al. Nucleic Acids Res, 2007. 35(11), 3581-9.
包装清单:
产品编号
|
产品名称
|
包装
|
SF1168-10mM
|
Pixantrone (topoisomerase II抑制剂)
|
10mM×0.2ml
|
SF1168-5mg
|
Pixantrone (topoisomerase II抑制剂)
|
5mg
|
SF1168-25mg
|
Pixantrone (topoisomerase II抑制剂)
|
25mg
|
—
|
说明书
|
1份
|
保存条件:
-20℃保存,至少一年有效。5mg和25mg包装也可室温保存,至少6个月有效。如果溶于非DMSO溶剂,建议分装后-80℃保存,预计6个月内有效。
注意事项:
本产品对人体有害,操作时请小心,并注意有效防护以避免直接接触人体或吸入体内。
本产品仅限于专业人员的科学研究用,不得用于临床诊断或治疗,不得用于食品或药品,不得存放于普通住宅内。
为了您的安全和健康,请穿实验服并戴一次性手套操作。