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| 10mg |
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Epirubicin (IMI 28; IMI-28; 4'-epidoxorubicin; epiADR; epidoxorubicin; Ellence; Pharmorubicin PFS) is an anthracycline-based anticancer agent used for chemotherapy. Patients with breast cancer who have undergone tumor excision surgery may benefit from the combination of epirubicin, a Topoisomerase inhibitor, and other medications.
| Targets |
Topoisomerase
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|---|---|
| ln Vitro |
Epirubicin (4'-Epidoxorubicin), like doxorubicin, exerts its antitumor effects by forming complexes with DNA that damage DNA and obstruct the synthesis of proteins, RNA, and DNA. The integrity and functionality of cellular membranes may also be impacted by epirubicin. Epirubicin's maximum cell killing happens in the S phase of the cell cycle. Effects are also observed in the early G2, G1, and M phases at higher concentrations[1].
Epirubicin display antineoplastic activity against most cancer cells. Hepatoma G2 cells exhibit cytotoxicity towards epirubicin, with an IC50 of 1.6 μg/mL after 24 hours. 1.6 micrograms per milliliter Hep G2 cells undergo apoptosis upon exposure to epirubicin, which also increases catalase activity by 50%, serine-dependent glutathione peroxidase activity by 110%, and the activity of Cu, Zn-superoxide dismutase by 172% and Mn-superoxide dismutase by 135%. Epirbicin decreases the expression of GST-π and increases the expression of NADPH-CYP 450 reductase in cells[3]. |
| ln Vivo |
Epirubicin (4'-Epidoxorubicin) exhibits clinical efficacy against a diverse array of tumor types, such as gastrointestinal cancer, head and neck cancer, ovarian cancer, prostatic carcinoma, transitional bladder carcinoma, breast cancer, malignant lymphomas, soft tissue sarcomas, lung cancer, pleural mesothelioma, and so forth[4].
For the human breast tumor xenograft R-27, epirubicin at a dose of 3.5 mg/kg reduces tumor mass by 74.4 %[5]. |
| Cell Assay |
In a 96-well plate, 500 monolayer Hep G2 cells are plated per well. Epirubicin is added to the medium and applied to the cells the following day. 15% of the MTT dye solution is added after the incubation times have passed. Each well receives an equal volume of solubilization/stop solution (dimethylsulfoxide) for an additional hour of incubation at 37°C following the first hour of incubation. At 570 nm, the absorbance of the reaction solution is measured and recorded.
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| References |
| Molecular Formula |
C₂₇H₂₉NO₁₁
|
|---|---|
| Molecular Weight |
543.52
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| Exact Mass |
543.17
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| Elemental Analysis |
C, 59.67; H, 5.38; N, 2.58; O, 32.38
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| CAS # |
56420-45-2
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| Related CAS # |
Epirubicin hydrochloride;56390-09-1
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| Appearance |
Solid powder
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| SMILES |
C[C@H]1[C@@H]([C@H](C[C@@H](O1)O[C@H]2C[C@@](CC3=C2C(=C4C(=C3O)C(=O)C5=C(C4=O)C(=CC=C5)OC)O)(C(=O)CO)O)N)O
|
| InChi Key |
AOJJSUZBOXZQNB-VTZDEGQISA-N
|
| InChi Code |
InChI=1S/C27H29NO11/c1-10-22(31)13(28)6-17(38-10)39-15-8-27(36,16(30)9-29)7-12-19(15)26(35)21-20(24(12)33)23(32)11-4-3-5-14(37-2)18(11)25(21)34/h3-5,10,13,15,17,22,29,31,33,35-36H,6-9,28H2,1-2H3/t10-,13-,15-,17-,22-,27-/m0/s1
|
| Chemical Name |
(7S,9S)-7-[(2R,4S,5R,6S)-4-amino-5-hydroxy-6-methyloxan-2-yl]oxy-6,9,11-trihydroxy-9-(2-hydroxyacetyl)-4-methoxy-8,10-dihydro-7H-tetracene-5,12-dione
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| Synonyms |
Epirubicin free base; IMI 28; IMI28; IMI-28; epi DX; 4-epiadriamycin; 4-epi DX; EPI; 4-epidoxorubicin; 4-epidoxorubicin HCl; epidoxorubicin; epiADR; epidorubicin; brand name: Ellence; Pharmorubicin PFS
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
|---|
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.8399 mL | 9.1993 mL | 18.3986 mL | |
| 5 mM | 0.3680 mL | 1.8399 mL | 3.6797 mL | |
| 10 mM | 0.1840 mL | 0.9199 mL | 1.8399 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
| NCT Number | Recruitment | interventions | Conditions | Sponsor/Collaborators | Start Date | Phases |
| NCT05084586 | Recruiting | Drug: Intravesical Solution | Bladder Cancer Tumor Recurrence |
Ankara Training and Research Hospital |
October 1, 2019 | Not Applicable |
| NCT05033808 | Recruiting | Drug: Epirubicin Drug: Placebo |
Sepsis | Jena University Hospital | October 19, 2022 | Phase 2 |
| NCT01740271 | Recruiting | Drug: Epirubicin | Breast Neoplasms | AHS Cancer Control Alberta | December 2012 | Phase 2 |
| NCT04576143 | Recruiting | Drug: Epirubicin Drug: Docetaxel |
HER2-negative Breast Cancer Neoadjuvant Chemotherapy |
Second Affiliated Hospital, School of Medicine, Zhejiang University |
September 20, 2020 | Phase 2 Phase 3 |
| NCT05121350 | Recruiting | Drug: Anlotinib hydrochloride capsule Drug: Epirubicin |
Soft Tissue Sarcoma | Chia Tai Tianqing Pharmaceutical Group Co., Ltd. |
March 2022 | Phase 3 |
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