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Epirubicin hydrochloride

CAS No. : 56390-09-1

MCE 国际站：Epirubicin hydrochloride

产品活性：Epirubicin hydrochloride (4'-Epidoxorubicin hydrochloride) 是阿霉素的半合成的 L-阿拉伯糖衍生物，能够抑制 Topoisomerase，起到抗肿瘤的作用。Epirubicin hydrochloride 抑制 DNA 和 RNA 合成。Epirubicin hydrochloride 是一种 Forkhead box 蛋白 p3 (Foxp3) 抑制剂，可抑制调节性 T 细胞活性。

研究领域：Cell Cycle/DNA Damage  |  Apoptosis  |  Anti-infection

作用靶点：DNA/RNA Synthesis  |  Topoisomerase  |  Apoptosis  |  Antibiotic

In Vitro: 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.

In Vivo: 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 %.

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