Epirubicin

目录号: GC35997纯度: >98%同义词: 表柔比星; 4'-Epidoxorubicin
Epirubicin是一种具有口服活性的DNA topoisomerase II特异性抑制剂,IC50为12μM。

Epirubicin
Cas No.: 56420-45-2
规格价格库存数量操作
5mg¥361.00现货
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10mg¥610.00现货
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25mg¥1,225.00现货
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50mg¥2,148.00现货
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100mg¥3,308.00现货
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10mM (in 1mL DMSO)¥460.00现货
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产品描述 Description

Epirubicin is an orally active, specific inhibitor of DNA topoisomerase II with an IC50 of 12μM[1]. Epirubicin forms a complex with DNA, blocks the re-ligation of DNA double strands, causes DNA damage, and interferes with DNA, RNA, and protein synthesis, thereby exerting broad-spectrum antitumor activity[2]. Epirubicin is commonly used in research on solid tumors such as breast, liver, and gastric cancers, as well as malignant lymphomas[3].

In vitro, Epirubicin (0.5-100μM; 48h) dose-dependently suppressed U-87 glioma cell proliferation, reduced MMP-9 secretion, lowered VEGF release, and inhibited cell migration[4]. Treatment of HCT116 and SW620 colorectal cancer cells with Epirubicin (125nM; 48h) significantly upregulated TRAIL and enhanced TRAIL-induced apoptosis[5].

In vivo, Epirubicin (2.5mg/kg; every other day for 16 days; i.v.) reduced tumor volume and increased tumor cell apoptosis in 4T1 breast cancer-bearing BALB/c mice[6]. Epirubicin (7mg/kg; every 4 days ×3; i.v.) reduced tumor massin R-27 human breast carcinoma-bearing nude mice without increasing toxic death[7].

References:
[1] 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.
[2] Luiz MT, Dutra JAP, Di Filippo LD, et al. Epirubicin: Biological Properties, Analytical Methods, and Drug Delivery Nanosystems. Crit Rev Anal Chem. 2023;53(5):1080-1093.
[3] Robert J. Clinical pharmacokinetics of epirubicin. Clin Pharmacokinet. 1994;26(6):428-438.
[4] Wang XF, Zhao ZF, Chen MH, Yuan QH, Li YL, Jiang CL. Epirubicin inhibits growth and alters the malignant phenotype of the U87 glioma cell line. Mol Med Rep. 2015;12(4):5917-5923.
[5] Caldiran F, Berkel C, Yilmaz E, et al. Combination treatment of bortezomib and epirubicin increases the expression of TNFRSF10 A/B, and induces TRAIL-mediated cell death in colorectal cancer cells. Biochem Biophys Res Commun. 2023;675:33-40.
[6] Wu J, Xue X, Zhang B, et al. Enhanced antitumor activity and attenuated cardiotoxicity of Epirubicin combined with Paeonol against breast cancer. Tumour Biol. 2016;37(9):12301-12313.
[7] Asanuma F, Yamada Y, Kawamura E, et al. Antitumor activity of paclitaxel and epirubicin in human breast carcinoma, R-27. Folia Microbiol (Praha). 1998;43(5):473-474.

Epirubicin是一种具有口服活性的DNA topoisomerase II特异性抑制剂,IC50为12μM[1]。Epirubicin与DNA形成复合物,阻断DNA双链的重新连接,导致DNA损伤,并干扰DNA、RNA及蛋白质合成,从而发挥广谱抗肿瘤活性[2]。Epirubicin常用于乳腺癌、肝癌、胃癌等实体瘤及恶性淋巴瘤的研究[3]

在体外,Epirubicin(0.5-100μM;48小时)可浓度依赖性地抑制U-87胶质瘤细胞增殖,减少MMP-9分泌,降低VEGF释放,并抑制细胞迁移[4]。Epirubicin(125nM;48小时)处理HCT116和SW620结直肠癌细胞后,显著上调TRAIL并增强TRAIL诱导的细胞凋亡[5]

在体内,Epirubicin(2.5mg/kg;隔日一次,持续16天;静脉注射)可减少4T1乳腺癌荷瘤BALB/c小鼠的肿瘤体积并增加肿瘤细胞凋亡[6]。Epirubicin(7mg/kg;每4天一次,共3次;静脉注射)在R-27人乳腺癌荷瘤裸鼠中降低肿瘤质量,且未增加毒性死亡[7]

实验参考方法 Experimental Reference Method

Cell experiment [1]:

Cell lines

human glioma cell line U-87

Preparation Method

The human glioma cell line U-87 cells were cultured in a standard tissue culture incubator (37˚C; 5% CO2; 95% air; 100% humidity). Cells were regularly passaged by treatment with trypsin (0.05%) and were grown in Eagle's minimum essential medium (EMEM) supplemented with 10% fetal bovine serum (FBS), penicillin and streptomycin, non-essential amino acids, 1mg/ml glucose and 1mM pyruvate. The U-87 and neuronal cells were plated on 96well flatbottomed microplates at a density of 1×104cells/well in 100µl complete growth medium. Prior to drug treatment, the growth medium was substituted with fresh medium containing 2% FBS. The U-87 and neuronal cells were exposed to Epirubicin at concentrations of 0.5-100µM. After 48h of incubation at 37˚C in a humidified atmosphere of 5% CO2, the cytotoxic effect of Epirubicin was estimated using an MTT assay. DNA synthesis in proliferating cells was evaluated by measuring Bromodeoxyuridine (BRDU) incorporation using a commercial Cell Proliferation ELISA System. MMP-9 levels in the conditioned media of the U-87 cells were determined using a commercial human MMP-9 immunoassay kit. Tumor cell migration was assessed using the wound healing assay.

Reaction Conditions

0.5-100µM; 48h

Applications

Epirubicin dose-dependently suppressed U-87 glioma cell proliferation, reduced MMP-9 secretion, and inhibited cell migration.

Animal experiment [2]:

Animal models

Female BALB/c mice

Preparation Method

Female BALB/c mice (8 weeks, weighting 18 to 22g) were housed in a specified chamber with controlled air conditions (temperature 20-25°C, humidity 50–65%) and free access to sterile food and water. A 4T1 cell suspension (100μL, 5×106cells/mL) was injected subcutaneously into the right side of the fourth mammary gland of each mouse. The tumor length (L) and width (W) were measured every other day, and the tumor volume was calculated by using the following formula: V (mm3)=(L×W2)/2. On day 8 of 4T1 cells injection, the size of tumors was approximately 100 mm3. Mice were randomly divided into two groups and accepted treatments every other day for eight times: Control group (Cont, n=8): mice received intragastrically administered (i.g.) and a tail intravenous injection of saline. Epirubicin group (n=8): mice received i.g. saline and a tail intravenous injection of Epirubicin (2.5mg/kg). The mice weights were recorded every other day. Blood was collected and the mice were sacrificed after 16 days. The tumors, hearts, and other tissues were removed rapidly and weighed. Several tissues were fixed in formalin for HE staining, TdT-mediated dUTP nick end labeling, and immunohistochemistry, whereas others were rapidly frozen in liquid nitrogen and stored in −80°C for Western blotting analysis.

Dosage form

2.5mg/kg; every other day for 16 days; i.v.

Applications

Epirubicin reduced tumor volume and increased tumor cell apoptosis in 4T1 breast cancer-bearing BALB/c mice.

References:
[1] Wang XF, Zhao ZF, Chen MH, Yuan QH, Li YL, Jiang CL. Epirubicin inhibits growth and alters the malignant phenotype of the U87 glioma cell line. Mol Med Rep. 2015;12(4):5917-5923.
[2] Wu J, Xue X, Zhang B, et al. Enhanced antitumor activity and attenuated cardiotoxicity of Epirubicin combined with Paeonol against breast cancer. Tumour Biol. 2016;37(9):12301-12313.

产品文档 Product Documents

化学性质Chemical Properties

CAS 号
56420-45-2
同义词
表柔比星; 4'-Epidoxorubicin
SMILES
O=C(C1=C2C(O)=C3[C@@H](O[C@@]4([H])C[C@H](N)[C@@H](O)[C@H](C)O4)C[C@@](C(CO)=O)(O)CC3=C1O)C5=CC=CC(OC)=C5C2=O
分子式
C27H29NO11
分子量
543.52 g/mol
溶解性
Soluble in DMSO
保存条件
Store at -20°C,protect from light
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Shipping Condition
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