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Epirubicin HCl

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Chemical Structure| 56390-09-1 同义名 : 盐酸表柔比星 ;4'-Epidoxorubicin hydrochloride;Epirubicin (hydrochloride);4’-Epidoxorubicin;4'-epidoxorubicin HCl;NSC 256942 HCl;IMI 28 HCl;Epirubicin hydrochloride
CAS号 : 56390-09-1
货号 : A263227
分子式 : C27H30ClNO11
纯度 : 99%+
分子量 : 579.98
MDL号 : MFCD00941448
存储条件：

粉末 Inert atmosphere,Store in freezer, under -20°C

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 25 mg/mL(43.1 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO

H2O: 50 mg/mL(86.21 mM)，配合低频超声助溶
动物实验配方：

PO 0.5% CMC-Na 12 mg/mL suspension

生物活性
靶点

  • Topoisomerase
描述 Epirubicin, a semisynthetic L-arabino derivative of doxorubicin, has an antineoplastic agent by inhibiting Topoisomerase[3]. Epirubicin inhibits DNA and RNA synthesis. Epirubicin is a Forkhead box protein p3 (Foxp3) inhibitor and inhibits regulatory T cell activity{ Kashima H, Momose F, Umehara H, et al. Epirubicin, Identified Using a Novel Luciferase Reporter Assay for Foxp3 Inhibitors, Inhibits Regulatory T Cell Activity. PLoS One. 2016;11(6):e0156643. |https://pubmed.ncbi.nlm.nih.gov/27284967/}}. Epirubicin is cytotoxic to Hepatoma G2 cells with IC50 of 1.6 μg/mL at 24 hr. 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%[4]. Epirubicin at a dose of 3.5 mg/kg suppresses tumor mass of human breast tumor xenograft R-27 by 74.4 %[5].
细胞研究
细胞系 浓度 检测类型 检测时间 活动说明 数据源
human A549 cells Proliferation assay 48 h Antiproliferative activity against human A549 cells after 48 hrs by MTT assay, IC50=9.6 μM 23287057
human DU145 cells Proliferation assay 48 h Antiproliferative activity against human DU145 cells after 48 hrs by MTT assay, IC50=9.9 μM 23287057
human HCT116 cells Cytotoxic assay 6 days Cytotoxicity against human HCT116 cells after 6 days by MTT assay, IC50=0.82 μM 22276679
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

1.72mL

0.34mL

0.17mL

8.62mL

1.72mL

0.86mL

17.24mL

3.45mL

1.72mL
参考文献

[1]Ozkan A, Fişkin K. Epirubicin HCl toxicity in human-liver derived hepatoma G2 cells. Pol J Pharmacol. 2004 Jul-Aug;56(4):435-44.

[2]Cersosimo RJ, Hong WK. Epirubicin: a review of the pharmacology, clinical activity, and adverse effects of an adriamycin analogue. J Clin Oncol. 1986 Mar;4(3):425-39.

[3]Cersosimo RJ, Hong WK. Epirubicin: a review of the pharmacology, clinical activity, and adverse effects of an adriamycin analogue. J Clin Oncol. 1986;4(3):425-439.

[4]Ozkan A, Fişkin K. Epirubicin HCl toxicity in human-liver derived hepatoma G2 cells. Pol J Pharmacol. 2004;56(4):435-444.

[5]Bonadonna G, Gianni L, Santoro A, et al. Drugs ten years later: epirubicin. Ann Oncol. 1993;4(5):359-369.