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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。

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

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%

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