盐酸表阿霉素作用机制 - Medchemexpress - MCE中国

1、Product Data SheetEpirubicin hydrochlorideCat. No.: HY-13624ACAS No.: 56390-09-1分式: CHClNO分量: 579.98作靶点: Topoisomerase; Apoptosis作通路: Cell Cycle/DNA Damage; Apoptosis储存式: 4C, protect from light* In solvent : -80C, 6 months; -20C, 1 month (protect from light)溶解性数据体外实验 DMSO : 103.3 mg/mL (178.11 mM)H2

2、O : 50 mg/mL (86.21 mM; Need ultrasonic)* means soluble, but saturation unknown.SolventMass1 mg 5 mg 10 mgConcentration制备储备液1 mM 1.7242 mL 8.6210 mL 17.2420 mL5 mM 0.3448 mL 1.7242 mL 3.4484 mL10 mM 0.1724 mL 0.8621 mL 1.7242 mL请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；旦配成溶液，请分装保存，避免反复冻融造成的产品失效。储备液的保存式和期限：-80C, 6

3、 months; -20C, 1 month (protect from light)。-80C 储存时，请在 6 个内使，-20C 储存时，请在 1 个内使。体内实验 请根据您的实验动物和给药式选择适当的溶解案。以下溶解案都请先按照 In Vitro 式配制澄清的储备液，再依次添加助溶剂：为保证实验结果的可靠性，澄 的储备液可以根据储存条件，适当保存；体内实验的作液，建议您现现配，当天 使； 以下溶剂前显的百分 指该溶剂在您配制终溶液中的体积占；如在配制过程中出现沉淀、析出现象，可 以通过加热和/或超声的式助溶1. 请依序添加每种溶剂： 10% DMSO 40% PEG300 5% Twee

4、n-80 45% salineSolubility: 2.58 mg/mL (4.45 mM); Clear solution此案可获得 2.58 mg/mL (4.45 mM，饱和度未知) 的澄清溶液。以 1 mL 作液为例，取 100 L 25.8 mg/mL 的澄 DMSO 储备液加到 400 L PEG300 中，混合均匀；向上述体系中加50 L Tween-80，混合均匀；然后继续加 450 L 理盐定容 1 mL。BIOLOGICAL ACTIVITYPage 1 of 2 www.MedChemE物活性 Epirubicin hydrochloride (4-Epidoxorub

5、icin hydrochloride) 阿霉素的半合成的 L-阿拉伯糖衍物，能够抑制 Topoisomerase，起到抗肿瘤的作。Epirubicin hydrochloride 种 Forkhead box 蛋 p3 (Foxp3) 抑制剂，可抑 制调节性 T 细胞活性。IC & Target Topoisomerase体外研究 Epirubicin hydrochloride (4-Epidoxorubicin hydrochloride), like doxorubicin, exerts its antitumor effects by complexwith DNA, resulti

6、ng in damage to DNA and interference with the synthesis of DNA, RNA, and proteins. Epirubicinhydrochloride may also affect the integrity and activity of cellular membranes. Maximal cell kill caused by Epirubicinhydrochloride occurs during the S phase of the cell cycle. With higher concentrations eff

7、ects are also seen in earlyG2 as well as G1 and M phases1.Epirubicin hydrochloride display antineoplastic activity against most cancer cells. Epirubicin hydrochloride iscytotoxic to Hepatoma G2 cells with IC50 of 1.6 g/mL at 24 hr. 1.6 g/mL Epirubicin hydrochloride inducesapoptosis of Hep G2 cells,

8、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 increasesthe cellular expression of NADPH-CYP 450 reductase, and reduces GST- expression3.体内研究 Epirubicin hydrochlorid

9、e (4-Epidoxorubicin hydrochloride) are clinically active against a broad range of tumortypes, including breast cancer, malignant lymphomas, soft tissue sarcomas, lung cancer, pleural mesothelioma, gastrointestinal cancer, head and neck cancer, ovarian cancer, prostatic carcinoma, transitional bladde

10、r carcinoma and so on4.Epirubicin hydrochloride at a dose of 3.5 mg/kg suppresses tumor mass of human breast tumor xenograft R-27 by74.4 %5.PROTOCOLCell Assay 3 Hep G2 cells (500 cells/well, monolayer) are plated in a 96-well plate. The next day the cells are treated with Epirubicinin the medium. At

11、 the end of the incubation periods, 15% volume of MTT dye solution is added. After 1 hr ofincubation at 37C, an equal volume of solubilization/stop solution (dimethylsul-foxide) is added to each well for anadditional 1 hr incubation. The absorbance of the reaction solution at 570 nm is recorded.MCE

12、has not independently confirmed the accuracy of these methods. They are for reference only.户使本产品发表的科研献 J Mol Med (Berl). 2019 Aug;97(8):1183-1193. Mol Pharm. 2019 Aug 5;16(8):3452-3459. Exp Cell Res. 2020 May 3:112054. Oncol Lett. 2020 Apr. Yonsei Med J. 2019 Sep;60(9):832-841.See more customer vali

13、dations on HYPERLINK www.MedChemE www.MedChemEREFERENCES1. Cersosimo RJ, et al. Epirubicin: a review of the pharmacology, clinical activity, and adverse effects of an adriamycin analogue. J Clin Oncol. 1986Mar;4(3):425-39.Page 2 of 3 www.MedChemE2. Ozkan, A., et al. Epirubicin HCl toxicity in human-

14、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. 473-4.5. Kashima H, et al. Epirubicin, Identified Using a Novel Luciferase Reporter Assay for Foxp3 Inhibitors, Inhibits Regulatory T Cell Activity. PLoS One. 2016Jun 10;11(6):e0156643.Mc