Epirubicin-hydrochloride-4-Epidoxorubicin-hydrochloride-DataSheet-生命科學(xué)試劑-MedChemExpress

1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemEEpirubicin hydrochlorideCat. No.: HY-13624ACAS No.: 56390-09-1Synonyms: 4-Epidoxorubicin hydrochloride分式: CHClNO分量: 579.98作靶點(diǎn): Topoisomerase作通路: Cell Cycle/DNA Damage儲存式: 4C, protect from light* In solvent : -80C, 6 months; -20C

2、, 1 month (protect fromlight)溶解性數(shù)據(jù)體外實(shí)驗(yàn) DMSO : 103.3 mg/mL (178.11 mM)H2O : 40% PEG300 5% Tween-80 45% salineSolubility: 2.58 mg/mL (4.45 mM); Clear solutionBIOLOGICAL ACTIVITY1/3 Master of Small Molecules 您邊的抑制劑師www.MedChemE物活性 Epirubicin hydrochloride阿霉素的半合成的 L-阿拉伯糖衍物，能夠抑制 Topoisomerase，起到抗腫瘤的作。IC5

3、0 & Target Topoisomerase體外研究 Epirubicin, like doxorubicin, exerts its antitumor effects by complex with DNA, resulting in damage to DNAand interference with the synthesis of DNA, RNA, and proteins. Epirubicin may also affect the integrity andactivity of cellular membranes. Maximal cell kill caused b

4、y Epirubicin occurs during the S phase of the cellcycle. With higher concentrations effects are also seen in early G2 as well as G1 and M phases1. Epirubicin display antineoplastic activity against most cancer cells. Epirubicin is cytotoxic to HepatomaG2 cells with IC50 of 1.6 g/mL at 24 hr. 1.6 g/m

5、L Epirubicin induces apoptosis of Hep G2 cells, and higheractivity of catalase by 50%, Se-dependent glutathione peroxidase by 110%, Cu, Zn-superoxide dismutase by172% and Mn-superoxide dismutase by 135%. Epirbicin increases the cellular expression of NADPH-CYP450 reductase, and reduces GST- expressi

6、on 2.體內(nèi)研究 Epirubicin are clinically active against a broad range of tumor types, including breast cancer, malignantlymphomas, soft tissue sarcomas, lung cancer, pleural mesothelioma, gastrointestinal cancer, head and neckcancer, ovarian cancer, prostatic carcinoma, transitional bladder carcinoma and

7、 so on 3. Epirubicin at adose of 3.5 mg/kg suppresses tumor mass of human breast tumor xenograft R-27 by 74.4 % 4.PROTOCOLCell Assay 3 Hep G2 cells (500 cells/well, monolayer) are plated in a 96-well plate. The next day the cells are treated withEpirubicin in the medium. At the end of the incubation

8、 periods, 15% volume of MTT dye solution is added.After 1 hr of incubation at 37C, an equal volume of solubilization/stop solution (dimethylsul-foxide) is addedto each well for an additional 1 hr incubation. The absorbance of the reaction solution at 570 nm is recorded.MCE has not independently conf

9、irmed the accuracy of these methods. They are for reference only.戶使本產(chǎn)品發(fā)表的科研獻(xiàn) J Mol Med (Berl). 2019 Jun 14. Mol Pharm. 2019 Jun.See more customer validations on HYPERLINK / www.MedChemEREFERENCES1. Cersosimo RJ, et al. Epirubicin: a review of the pharmacology, clinical activity, and adverse effects

10、of an adriamycin analogue. J ClinOncol. 1986 Mar;4(3):425-39.2. Ozkan, A., et al. Epirubicin HCl toxicity in human-liver derived hepatoma G2 cells. Pol J Pharmacol, 2004. 56(4): p. 435-44.3. Bonadonna, G., et al. Drugs ten years later: epirubicin. Ann Oncol, 1993. 4(5): p. 359-69.4. Asanuma, F., et al. Antitumor activity of paclitaxel and epirubicin in human breast carcinoma, R-27. Folia Microbiol (Praha), 1998. 43(5):p. 473-4.2/3 Master of Small Molecules 您邊的抑制劑師www.MedChemEMcePdfHeightCaution: Product has not been f