| CAS NO: | 56390-09-1 |
| 包装 | 价格(元) |
| 10mM (in 1mL DMSO) | 电议 |
| 5mg | 电议 |
| 25mg | 电议 |
| 100mg | 电议 |
| Physical Appearance | A solid |
| Storage | Store at -20°C |
| M.Wt | 579.98 |
| Cas No. | 56390-09-1 |
| Formula | C27H29NO11·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 |
| Canonical SMILES | CC1C(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 |
| 运输条件 | 蓝冰运输或根据您的需求运输。 |
| 一般建议 | 为了使其更好的溶解，请用37℃加热试管并在超声波水浴中震动片刻。不同厂家不同批次产品溶解度各有差异，仅做参考。若实验所需浓度过大至产品溶解极限，请添加助溶剂助溶或自行调整浓度。溶液形式一般不宜长期储存，请尽快用完。 |
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.
| 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, Fiskin 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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