Epirubicin hydrochloride

SKU: orb1224651

Description

Epirubicin hydrochloride, a semisynthetic L-arabino derivative of doxorubicin, is an antineoplastic agent by inhibiting Topoisomerase.(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 %.

Key Properties

• CAS Number: 56390-09-1
• MW: 579.98
• Purity: >98% (HPLC)
• Formula: C₂₇H₃₀ClNO₁₁
• SMILES: C[C@H]1[C@@H]([C@H](C[C@@H](O1)O[C@H]2C[C@@](CC3=C(C4=C(C(=C23)O)C(=O)C5=C(C4=O)C=CC=C5OC)O)(C(=O)CO)O)N)O.Cl
• Target: Topoisomerase
• Solubility: Water: 100 mg/mL warmed (172.41 mM); DMSO: 100 mg/mL (172.41 mM)

Bioactivity

• 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 %.
• 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.

Storage & Handling

• Storage: Storage temperature: -20°C. Stability: ≥ 2 years
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

4’-Epidoxorubicin

Quick Database Links

Gene Symbol

Topoisomerase