产品
编 号:F391253
分子式:C27H30ClNO11
分子量:579.98
产品类型
结构图
CAS No: 56390-09-1
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产品详情
生物活性:
Epirubicin hydrochloride (4'-Epidoxorubicin hydrochloride), a semisynthetic L-arabino derivative of doxorubicin, has an antineoplastic agent by inhibiting Topoisomerase. Epirubicin hydrochloride inhibits DNA and RNA synthesis. Epirubicin hydrochloride is a Forkhead box protein p3 (Foxp3) inhibitor and inhibits regulatory T cell activity.
体内研究:
Epirubicin hydrochloride (4'-Epidoxorubicin hydrochloride) are clinically active against a broad range of tumor types, including breast cancer, malignant lymphomas, soft tissue sarcomas, lung cancer, pleural mesothelioma, gastrointestinal cancer, head and neck cancer, ovarian cancer, prostatic carcinoma, transitional bladder carcinoma and so on. Epirubicin hydrochloride at a dose of 3.5 mg/kg suppresses tumor mass of human breast tumor xenograft R-27 by 74.4 %.
体外研究:
Epirubicin hydrochloride (4'-Epidoxorubicin hydrochloride), like doxorubicin, exerts its antitumor effects by complex with DNA, resulting in damage to DNA and interference with the synthesis of DNA, RNA, and proteins. Epirubicin hydrochloride may also affect the integrity and activity of cellular membranes. Maximal cell kill caused by Epirubicin hydrochloride occurs during the S phase of the cell cycle. With higher concentrations effects are also seen in early G2 as well as G1 and M phases. Epirubicin hydrochloride display antineoplastic activity against most cancer cells. Epirubicin hydrochloride is cytotoxic to Hepatoma G2 cells with IC50 of 1.6 μg/mL at 24 hr. 1.6 μg/mL Epirubicin hydrochloride induces apoptosis of Hep G2 cells, and higher activity of catalase by 50%, Se-dependent glutathione peroxidase by 110%, Cu, Zn-superoxide dismutase by 172% and Mn-superoxide dismutase by 135%. Epirubicin hydrochloride increases the cellular expression of NADPH-CYP 450 reductase, and reduces GST-π expression.