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盐酸依达比星

盐酸依达比星用途

Idarubicin hydrochloride是一种蒽环类抗白血病药物。它抑制拓扑异构酶II,干扰DNA复制和RNA转录。

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盐酸依达比星名称

[ CAS 号 ]:
57852-57-0

[ 中文名 ]:
盐酸依达比星

[ 英文名 ]:
Idarubicin (hydrochloride)

[中文别名 ]:

[英文别名 ]:

4-demethoxy-daunomycihydrochloride
4-DMD HCl
Idarubicin hcl USP/EP
IdarubicinHCl
4-demethoxydaunomycin hydrochloride
Idarubicin HCl
Idamycin
Zavedos
Idarubicin HCL for research
IDARUBICIN HYDROCHLORIDE

盐酸依达比星生物活性

[ 描述 ]:

Idarubicin hydrochloride是一种蒽环类抗白血病药物。它抑制拓扑异构酶II,干扰DNA复制和RNA转录。

[ 相关类别 ]:

信号通路 >> 自噬 >> 自噬

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 II

[体外研究]

伊达比星的IC50在MCF-7单层上为3.3±0.4 ng/mL,在多细胞球体中为7.9±1.1 ng/mL [1]。在各种体外系统中,Idarubicin比柔红霉素或多柔比星显示出更大的细胞毒性。这归因于伊达比星更好地诱导拓扑异构酶II介导的DNA断裂的形成[2]。伊达比星的活性分别比阿霉素和表柔比星高约57.5倍和25倍[3]。 Idarubicin产生浓度依赖性细胞生长减少,IC50值约为0.01μM。 Idarubicin产生浓度依赖性的DNA合成抑制[4]。

[细胞实验]

将盐酸伊达比星的储备溶液溶解在蒸馏水（1mg / mL）中。将MCF-7单层以0.01,0.1,1,10,100和1000ng / mL暴露于伊达比星或其代谢物伊达比星，持续24小时。多细胞球体暴露于相同范围的伊达比星和伊达比星浓度单层（0.01-1000 ng / mL）24小时，并且在单独的实验中，药物浓度为100 ng / mL，持续6,12,24和48小时。通过用血细胞计数器计数活细胞来确定细胞增殖的抑制。结果表示为细胞存活与对照培养物的百分比[1]。

[参考文献]

[1]. Orlandi P, et al. Idarubicin and idarubicinol effects on breast cancer multicellular spheroids. J Chemother. 2005 Dec;17(6):663-7.

[2]. Robert J. Clinical pharmacokinetics of idarubicin. Clin Pharmacokinet. 1993 Apr;24(4):275-88.

[3]. Siegsmund MJ, et al. Enhanced in vitro cytotoxicity of idarubicin compared to epirubicin and doxorubicin in rat prostate carcinoma cells. Eur Urol. 1997;31(3):365-70.

[4]. Gewirtz DA, et al. Induction of DNA damage, inhibition of DNA synthesis and suppression of c-myc expression by the anthracycline analog, idarubicin (4-demethoxy-daunorubicin) in the MCF-7 breast tumor cell line. Cancer Chemother Pharmacol. 1998;41(5):361-

[相关活性小分子]

盐酸依达比星物理化学性质

[ 沸点 ]:
725.4ºC at 760 mmHg

[ 熔点 ]:
183-185ºC

[ 分子式 ]:
C₂₆H₂₈ClNO₉

[ 分子量 ]:
533.955

[ 闪点 ]:
392.5ºC

[ 精确质量 ]:
533.145264

[ PSA ]:
176.61000

[ LogP ]:
2.52260

[ 外观性状 ]:
粉末

[ 储存条件 ]:
-20℃

盐酸依达比星毒性和生态

CHEMICAL IDENTIFICATION

RTECS NUMBER :: HB7877000

CHEMICAL NAME :: Daunomycin, 4-demethoxy-, hydrochloride

CAS REGISTRY NUMBER :: 57852-57-0

LAST UPDATED :: 199612

DATA ITEMS CITED :: 8

MOLECULAR FORMULA :: C26-H27-N-O9.Cl-H

MOLECULAR WEIGHT :: 534.00

WISWESSER LINE NOTATION :: L E6 C666 BV MVT&&&J DQ FQ HV1 HQ KQ RQ

HEALTH HAZARD DATA

ACUTE TOXICITY DATA

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

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 5430 ug/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: 26,364,1995

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

ROUTE OF EXPOSURE :: Subcutaneous

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 2930 ug/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: 26,364,1995

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

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 3080 ug/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: 26,364,1995

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

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 13980 ug/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: 26,364,1995

TYPE OF TEST :: LDLo - Lowest published lethal dose

ROUTE OF EXPOSURE :: Intraperitoneal

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 700 ug/kg

TOXIC EFFECTS :: Tumorigenic - active as anti-cancer agent

REFERENCE :: CTRRDO Cancer Treatment Reports. (Washington, DC) V.60-71, 1976-87. For publisher information, see JNCIEQ. Volume(issue)/page/year: 60,829,1976

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

ROUTE OF EXPOSURE :: Subcutaneous

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 4690 ug/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: 26,364,1995

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

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 4100 ug/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: 26,364,1995

TYPE OF TEST :: LD - Lethal dose

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Mammal - dog

DOSE/DURATION :: >500 ug/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: 26,364,1995

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盐酸依达比星安全信息

[ 符号 ]:

GHS06, GHS08

[ 信号词 ]:
Danger

[ 危害声明 ]:
H300-H351-H360

[ 警示性声明 ]:
P201-P264-P281-P301 + P310-P308 + P313

[ 个人防护装备 ]:
Eyeshields;Faceshields;full-face particle respirator type N100 (US);Gloves;respirator cartridge type N100 (US);type P1 (EN143) respirator filter;type P3 (EN 143) respirator cartridges

[ 危害码 (欧洲) ]:
T+:Verytoxic;

[ 风险声明 (欧洲) ]:
R60;R61;R28;R40

[ 安全声明 (欧洲) ]:
S53-S45

[ 危险品运输编码 ]:
UN 2811

[ RTECS号 ]:
HB7877000

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