< 生产厂家价格 >

盐酸表柔比星

盐酸表柔比星用途

Epirubicin hydrochloride 是阿霉素的半合成的 L-阿拉伯糖衍生物,能够抑制 Topoisomerase,起到抗肿瘤的作用。

点击显示

盐酸表柔比星名称

[ CAS 号 ]:
56390-09-1

[ 中文名 ]:
盐酸表柔比星

[ 英文名 ]:
Epirubicin hydrochloride

[中文别名 ]:

盐酸表阿霉素

[英文别名 ]:

Pidorubicin hydrochloride
Ellence
Epirubicin hydrochloride
EINECS 260-145-2
EPIRUBICIN HCl
Epirubicin (hydrochloride)

盐酸表柔比星生物活性

[ 描述 ]:

Epirubicin hydrochloride 是阿霉素的半合成的 L-阿拉伯糖衍生物,能够抑制 Topoisomerase,起到抗肿瘤的作用。

[ 相关类别 ]:

信号通路 >> 细胞周期/DNA损伤 >> 拓扑异构酶

研究领域 >> 癌症

[ 靶点 ]

Topoisomerase

[体外研究]

与阿霉素一样,表柔比星通过与DNA的复合物发挥其抗肿瘤作用,导致DNA损伤并干扰DNA,RNA和蛋白质的合成。表柔比星也可能影响细胞膜的完整性和活性。表柔比星引起的最大细胞杀伤发生在细胞周期的S期。随着浓度的增加,早期G2以及G1期和M期也会出现影响[1]。表柔比星显示出对抗大多数癌细胞的抗肿瘤活性。表柔比星对肝癌G2细胞具有细胞毒性,24小时IC50为1.6μg/ mL。 1.6μg/ mL表阿霉素诱导Hep G2细胞凋亡,过氧化氢酶活性增加50％,Se依赖型谷胱甘肽过氧化物酶活性增加110％,Cu,Zn超氧化物歧化酶增加172％,Mn-超氧化物歧化酶增加135％。 Epirbicin可增加NADPH-CYP 450还原酶的细胞表达,并降低GST-π的表达[2]。

[体内研究]

表柔比星对多种肿瘤类型具有临床活性,包括乳腺癌,恶性淋巴瘤,软组织肉瘤,肺癌,胸膜间皮瘤,胃肠癌,头颈癌,卵巢癌,前列腺癌,膀胱移行癌等[ 3]。剂量为3.5mg/kg的表柔比星抑制人乳腺肿瘤异种移植物R-27的肿瘤质量达74.4％[4]。

[细胞实验]

将Hep G2细胞（500个细胞/孔，单层）接种在96孔板中。第二天，在培养基中用表柔比星处理细胞。在孵育期结束时，加入15％体积的MTT染料溶液。在37℃温育1小时后，向每个孔中加入等体积的溶解/终止溶液（二甲基亚砜 - 氧化物），再孵育1小时。记录反应溶液在570nm处的吸光度。

[参考文献]

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

[2]. Ozkan, A., et al. Epirubicin HCl toxicity in human-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.

[相关活性小分子]

盐酸表柔比星物理化学性质

[ 密度 ]:
1.61g/cm3

[ 沸点 ]:
810.3ºC at 760 mmHg

[ 熔点 ]:
185ºC dec

[ 分子式 ]:
C₂₇H₃₀ClNO₁₁

[ 分子量 ]:
579.980

[ 闪点 ]:
443.8ºC

[ 精确质量 ]:
579.150757

[ PSA ]:
206.07000

[ LogP ]:
1.50360

[ 外观性状 ]:
橙色-红色结晶固体

[ 折射率 ]:
1.709

[ 储存条件 ]:
2~8°C，干燥，密封

盐酸表柔比星毒性和生态

CHEMICAL IDENTIFICATION

RTECS NUMBER :: QI9295750

CHEMICAL NAME :: 5,12-Naphthacenedione, 10-((3-amino-2,3,6-trideoxy-alpha-L-arabino-hexopyran osyl)oxy)- 7,8,9,10-tetrahydro-6,8,11-trihydroxy-8-(hydroxyacety l)-1-methoxy-, hydrochloride, (8S-cis)-

CAS REGISTRY NUMBER :: 56390-09-1

LAST UPDATED :: 199612

DATA ITEMS CITED :: 9

MOLECULAR FORMULA :: C27-H29-N-O11.Cl-H

MOLECULAR WEIGHT :: 580.03

HEALTH HAZARD DATA

ACUTE TOXICITY DATA

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Human - woman

DOSE/DURATION :: 1622 mg/kg

TOXIC EFFECTS :: Sense Organs and Special Senses (Eye) - effect, not otherwise specified Gastrointestinal - changes in structure or function of salivary glands Immunological Including Allergic - uncharacterized

REFERENCE :: LANCAO Lancet. (7 Adam St., London WC2N 6AD, UK) V.1- 1823- Volume(issue)/page/year: 2,629,1986

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 1350 mg/kg

TOXIC EFFECTS :: Details of toxic effects not reported other than lethal dose value

REFERENCE :: NIIRDN Drugs in Japan (Ethical Drugs). (Yakugyo Jiho Co., Ltd., Tokyo, Japan) Volume(issue)/page/year: -,200,1990

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Intraperitoneal

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 10800 ug/kg

TOXIC EFFECTS :: Details of toxic effects not reported other than lethal dose value

REFERENCE :: NIIRDN Drugs in Japan (Ethical Drugs). (Yakugyo Jiho Co., Ltd., Tokyo, Japan) Volume(issue)/page/year: -,200,1990

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Subcutaneous

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 17600 ug/kg

TOXIC EFFECTS :: Details of toxic effects not reported other than lethal dose value

REFERENCE :: NIIRDN Drugs in Japan (Ethical Drugs). (Yakugyo Jiho Co., Ltd., Tokyo, Japan) Volume(issue)/page/year: -,200,1990

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 17 mg/kg

TOXIC EFFECTS :: Details of toxic effects not reported other than lethal dose value

REFERENCE :: IYKEDH Iyakuhin Kenkyu. Study of Medical Supplies. (Nippon Koteisho Kyokai, 12-15, 2-chome, Shibuya, Shibuya-ku, Tokyo 150, Japan) V.1- 1970- Volume(issue)/page/year: 26,740,1995

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: >2 gm/kg

TOXIC EFFECTS :: Details of toxic effects not reported other than lethal dose value

REFERENCE :: NIIRDN Drugs in Japan (Ethical Drugs). (Yakugyo Jiho Co., Ltd., Tokyo, Japan) Volume(issue)/page/year: -,200,1990

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Subcutaneous

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 37500 ug/kg

TOXIC EFFECTS :: Details of toxic effects not reported other than lethal dose value

REFERENCE :: NIIRDN Drugs in Japan (Ethical Drugs). (Yakugyo Jiho Co., Ltd., Tokyo, Japan) Volume(issue)/page/year: -,200,1990

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 31500 ug/kg

TOXIC EFFECTS :: Details of toxic effects not reported other than lethal dose value

REFERENCE :: NIIRDN Drugs in Japan (Ethical Drugs). (Yakugyo Jiho Co., Ltd., Tokyo, Japan) Volume(issue)/page/year: -,200,1990

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Mammal - dog

DOSE/DURATION :: 2250 ug/kg

TOXIC EFFECTS :: Details of toxic effects not reported other than lethal dose value

REFERENCE :: NIIRDN Drugs in Japan (Ethical Drugs). (Yakugyo Jiho Co., Ltd., Tokyo, Japan) Volume(issue)/page/year: -,200,1990

点击显示

盐酸表柔比星安全信息

[ 符号 ]:

GHS07, GHS08

[ 信号词 ]:
Danger

[ 危害声明 ]:
H302-H340-H350-H360

[ 警示性声明 ]:
P201-P280-P301 + P312 + P330-P308 + P313

[ 危害码 (欧洲) ]:
Xn

[ 风险声明 (欧洲) ]:
22-63-62-46-40

[ 安全声明 (欧洲) ]:
36/37/38-45-46

[ 危险品运输编码 ]:
NONH for all modes of transport

[ RTECS号 ]:
QI9295750

[ 海关编码 ]:
2932999099

盐酸表柔比星海关

[ 海关编码 ]: 2932999099

[ 中文概述 ]:
2932999099. 其他仅含氧杂原子的杂环化合物. 增值税率:17.0%. 退税率:13.0%. 监管条件:无. 最惠国关税:6.5%. 普通关税:20.0%

[ 申报要素 ]: 品名, 成分含量, 用途

[ Summary ]:
2932999099. other heterocyclic compounds with oxygen hetero-atom(s) only. VAT:17.0%. Tax rebate rate:13.0%. . MFN tariff:6.5%. General tariff:20.0%

盐酸表柔比星文献

Fourier transform infrared spectroscopy imaging of live epithelial cancer cells under non-aqueous media.

J. Clin. Pathol. 66(4) , 312-8, (2013)

Fourier transform infrared (FT-IR) imaging is increasingly being applied to biomedical specimens, but strong IR absorption by water complicates live cell imaging. This study investigates the viability...

Intraabdominal follicular dendritic cell sarcoma: a report of three cases and review of the literature.

Tumori 99(2) , e65-9, (2013)

Follicular dendritic cell sarcoma (FDCS) is a rare neoplasm that originates from follicular dendritic cells in lymphoid follicles. FDCS has been increasingly reported in recent years. However, data on...

Treatment outcome in children and adolescents with relapsed Hodgkin lymphoma--results of the UK HD3 relapse treatment strategy.

Br. J. Haematol. 165(4) , 534-44, (2014)

The purpose of this national retrospective study was to evaluate the outcome in children with relapsed or primary refractory Hodgkin lymphoma [HL] after a primary chemotherapy alone treatment strategy...

更多文献