Epirubicin HCl

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Biological Activity

Description	Epirubicin HCl, a semisynthetic L-arabino derivative of doxorubicin, is an antineoplastic agent by inhibiting Topoisomerase.
Targets
IC50
In vitro	Epirubicin, 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 may also affect the integrity and activity of cellular membranes. Maximal cell kill caused by Epirubicin 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. [1] 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. [2]
In vivo	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. [3] Epirubicin at a dose of 3.5 mg/kg suppresses tumor mass of human breast tumor xenograft R-27 by 74.4 %. [4]
Features

Protocol(Only for Reference)

Cell Assay: ^[2]

Cell lines	Human hepatocellular carcinoma cell Hep G2
Concentrations	0.05-12 μg/mL
Incubation Time	1 days
Method	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.

Animal Study: ^[4]

Animal Models	Human breast tumor xenograft R-27
Dosages	3.5 mg/kg
Administration	i.v. every 4 day for 3 times
Solubility	30% PEG400/0.5% Tween80/5% propylene glycol 30 mg/mL

1

References

Clinical Trial Information( data from http://clinicaltrials.gov)

NCT Number	Recruitment	Conditions	Sponsor /Collaborators	Start Date	Phases
NCT01936064	Recruiting	Haematological Abnormality	Lagos State University	2013-09	Phase 1|Phase 2
NCT01855828	Recruiting	Her2-Positive Breast Cancer	Yale University|Lajos Pusztai|Genentech	2013-09	Phase 2
NCT01964027	Not yet recruiting	Stage IV Gastric Cancer With Metastasis	Anhui Medical University	2013-10	Phase 2
NCT02005783	Recruiting	Grade 3/4 Neutropenia|Febrile Neutropenia	Shanghai Jiao Tong University School of Medicine	2013-10	Phase 2
NCT01929811	Recruiting	pCR Rate|BCT Rate|Safety	Shanghai Jiao Tong University School of Medicine	2013-10	Phase 2

Chemical Information

Download Epirubicin HCl SDF

Chemical Name

Preparing Stock Solutions

Stock Solution (1ml DMSO)	1mM	10mM	20mM	30mM
Mass(mg)	0.57998	5.7998	11.5996	17.3994

Customer Reviews (1)

Click to enlarge	Rating
	Source	Dr. Edita Aksamitiene from Thomas Jefferson University.Epirubicin HCl purchased from Selleck
	Method	Cell viability assay
	Cell Lines	pancreatic cancer cells
	Concentrations	0-25 μM
	Incubation Time	48 h
	Results	Epirubicin potently inhibited the survival of MiaPaCa-2 cells in a dose-dependent manner.