货号: | R11015 |
CAS号: | 56390-09-1 |
供应商: | 上海芮晖化工 |
数量: | 大量 |
英文名: | Epirubicin hydrochloride |
保质期: | 两年 |
保存条件: | 冷冻 |
规格: | 10mg/25mg/100mg |
Epirubicin hydrochloride (盐酸表柔比星) 是半合成的doxorubicin衍生物,能通过抑制拓扑异构酶起到抗肿瘤的作用。
生物活性
Epirubicin Hcl, a semisynthetic L-arabino derivative of doxorubicin, is an antineoplastic agent by inhibiting Topoisomerase.
Target: Topoisomerase
Approved: 1999
Epirubicin display antineoplastic activity against most cancer cells. Epirubicin is cytotoxic to Hepatoma G2 cells with IC50 of 1.6 μg/mL at 24hr. 1.6 μg/mL Epirubicin 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%. Epirbicin increases the cellular expression of NADPH-CYP 450 reductase, and reduces GST-π expression [1].
Epirubicin 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 [2]. Epirubicin at a dose of 3.5 mg/kg suppresses tumor mass of human breast tumor xenograft R-27 by 74.4 % [3].
Toxicity: Bone marrow aplasia, grade 4 mucositis, and gastrointestinal bleeding
化学信息
分子量 | 579.98 | 储存条件 | 参考CoA中推荐的条件进行储存。 |
---|---|---|---|
分子式 | C₂₇H₃₀ClNO₁₁ | ||
CAS号 | 56390-09-1 | ||
溶剂/溶解度 | 10 mM in DMSO |
相关文献
[1]. Ozkan, A. and K. Fiskin, Epirubicin HCl toxicity in human-liver derived hepatoma G2 cells. Pol J Pharmacol, 2004. 56(4): p. 435-44.
[2]. Bonadonna, G., et al., Drugs ten years later: epirubicin. Ann Oncol, 1993. 4(5): p. 359-69.
[3]. Asanuma, F., et al., Antitumor activity of paclitaxel and epirubicin in human breast carcinoma, R-27. Folia Microbiol (Praha), 1998. 43(5): p. 473-4.