Epirubicin hydrochloride 是一种阿霉素的半合成 L-阿拉伯糖衍生物,是一种 Forkhead box 蛋白 p3 抑制剂,可抑制调节性 T 细胞活性。它抑制 DNA 和 RNA 合成,还能够抑制拓扑异构酶,起抗肿瘤作用。
产品描述
Epirubicin hydrochloride is an antineoplastic agent which can inhibit Topoisomerase.
体外活性
在3.5 mg/kg剂量下,Epirubicin可以抑制74.4%人类乳腺肿瘤异种移植的R-27的肿瘤块.Epirubicin对很多类型的肿瘤具有临床活性,包括乳腺癌,恶性淋巴瘤,软组织肉瘤,肺癌,胸膜间皮瘤,胃肠癌,头颈癌,卵巢癌,前列腺癌,移行膀胱癌等.
体内活性
Epirubicin对大多数癌细胞表现出抗肿瘤活性。1.6 μg/mL Epirubicin引起Hep G2细胞凋亡,使过氧化氢酶活性、Se-依赖性谷胱甘肽过氧化物酶活性、Cu,Zn-超氧化物歧化酶活性和Mn-超氧化物歧化酶活性分别提高50%,110%,172%和135%。Epirbicin增加NADPH-CYP 450还原酶在细胞中的表达,并减少GST-π的表达。
细胞实验
Hep G2 cells (500 cells/well, monolayer) are plated in a 96-well plate. The next day the cells are treated with Epirubicin in the medium. At the end of the incubation periods, 15% volume of MTT dye solution is added. After 1 hr of incubation at 37℃, an equal volume of solubilization/stop solution (dimethylsul-foxide) is added to each well for an additional 1 hr incubation. The absorbance of the reaction solution at 570 nm is recorded.(Only for Reference)
Cas No.
56390-09-1
分子式
C27H30ClNO11
分子量
579.98
别名
Pharmorubicin;4'-Epidoxorubicin hydrochloride;盐酸表柔比星;Epirubicin HCl;4'-epidoxorubicin HCl
储存和溶解度
Ethanol:5.8 mg/mL (10 mM)
DMSO:58 mg/mL (100 mM)
Powder: -20°C for 3 years
In solvent: -80°C for 2 years