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Epirubicin HCl

盐酸表阿霉素
Catalog No.
A2451
抗生素类抗肿瘤药物
组合的产品项目
规格价格库存 数量
10mM (in 1mL DMSO)
¥ 581.00
现货
5mg
¥ 409.00
现货
25mg
¥ 1,636.00
现货
100mg
¥ 3,272.00
现货

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A

背景

Epirubicin是一种DNA拓朴异构酶(TOPII)抑制剂[1]。

Epirubicin属于Anthracylines化学家族,是一种DNA拓朴异构酶抑制剂。Epirubicin可抑制DNA拓扑异构的再连接途径,导致5’磷酸-DNA复合体(剪切复合体)稳定化。这些损伤具有细胞毒性,可引起DNA损伤应答激活,并可能导致细胞凋亡。因此,Epirubicin通常用于癌症治疗。不幸的是,Epirubicin也存在遗传毒性副作用,包括可引发白血病的染色体易位形成[1]。

Epirubicin是一种用于治疗骨肉瘤的化疗剂。Epirubicin可通过诱发细胞凋亡,抑制肿瘤生长。相反地,Epirubicin可在OS细胞中通过活化NF-κB减少细胞凋亡。据报道,epirubicin与浅蓝菌素结合后可提高体内和体外的抗肿瘤活性[2]。

参考文献:
[1] Ian G.  Cowell, Caroline A. Austin. Mechanism of Generation of Therapy Related Leukemia in Response to Anti-Topoisomerase II Agents. International Journal of Environmental Research and Public Health. 2012 (9): 2075-2091.
[2] Z. L. LIU, G. WANG, Y. SHU, P.A. ZOU, Y. ZHOU and Q.S. YIN. Enhanced antitumor activity of epirubicin combined with cerulenin in osteosarcoma. Molecular Medicine Reports. 2012 (5): 326-330.

化学属性

Physical AppearanceA solid
StorageStore at -20°C
M.Wt579.98
Cas No.56390-09-1
FormulaC27H29NO11·HCl
Solubility≥29.00 mg/mL in DMSO; ≥10.12 mg/mL in EtOH with gentle warming and ultrasonic; ≥40.33 mg/mL in H2O with gentle warming
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;hydrochloride
SDFDownload SDF
Canonical SMILESCC1C(C(CC(O1)OC2CC(CC3=C(C4=C(C(=C23)O)C(=O)C5=C(C4=O)C=CC=C5OC)O)(C(=O)CO)O)N)O.Cl
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试验操作

Cell experiment:[1]

Cell lines

Human-liver derived hepatoma G2 cells (Hep G2 cells)

Reaction Conditions

0 ~ 12 μg/ml epirubicin HCl for 24, 48 or 72 h incubation

Applications

Epirubicin HCl produced a concentration- and time-dependent cytotoxicity to Hep G2 cells. The mechanism of cytotoxicity of epirubicin HCl (IC50 value of 1.6 μg/ml within 24 h) appeared to involve a production of free radical species since activities of free radical scavenging enzymes (SOD, catalase, Se-dependent GPx) were increased.

Animal experiment:[2]

Animal models

Nude mice xenografted with human breast carcinoma cell line R-27

Dosage form

3.5 or 7 mg/kg

Administered intravenously every 4 d for 3 times

Applications

Epirubicin treatment alone suppressed tumor growth in a dose-dependent manner. At a dose of 3.5 mg/kg, epirubicin alone suppressed tumor mass of human breast tumor xenograft R-27 by 74.4 %.

Note

The technical data provided above is for reference only.

References:

1. Ozkan A, Fişkin K. Epirubicin HCl toxicity in human-liver derived hepatoma G2 cells. Polish Journal of Pharmacology, 2004, 56(4): 435-444.

2. Asanuma F, Yamada Y, Kawamura E, et al. Antitumor activity of paclitaxel and epirubicin in human breast carcinoma, R-27. Folia Microbiologica (Praha), 1998, 43(5): 473-474.

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