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盐酸依达比星

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更新时间：2024-04-27 09:12:50

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常用名

盐酸依达比星

英文名

Idarubicin HCl
CAS号

57852-57-0

分子量

533.955
密度

N/A

沸点

725.4ºC at 760 mmHg
分子式

C₂₆H₂₈ClNO₉

熔点

183-185ºC
MSDS

闪点

392.5ºC
符号

GHS06

GHS08

信号词

Danger

盐酸依达比星名称

中文名

盐酸依达比星
英文名

Idarubicin HCl
中文别名

盐酸伊达比星 |盐酸雷洛昔芬 |
英文别名

(1S,3S)-3-Acetyl-3,5,12-trihydroxy-6,11-dioxo-1,2,3,4,6,11-hexahydro-1-tetracenyl 3-amino-2,3,6-trideoxy-α-L-lyxo-hexopyranoside hydrochloride (1:1) |4-demethoxy-daunomycihydrochloride |4-DMD HCl |(1S,3S)-3-Acetyl-1,2,3,4,6,11-hexahydro-3,5,12-trihydroxy-6,11-dioxo-1-naphthacenyl 3-amino-2,3,6-trideoxy-α-L-lyxo-hexopyranoside, hydrochloride |5,12-naphthacenedione, 9-acetyl-7-[(3-amino-2,3,6-trideoxy-α-L-lyxo-hexopyranosyl)oxy]-7,8,9,10-tetrahydro-6,9,11-trihydroxy-, (7S,9S)-, hydrochloride |Idarubicin hcl USP/EP |IdarubicinHCl |4-demethoxydaunomycin hydrochloride |Idarubicin HCl |5,12-Naphthacenedione, 9-acetyl-7-[(3-amino-2,3,6-trideoxy-α-L-lyxo-hexopyranosyl)oxy]-7,8,9,10-tetrahydro-6,9,11-trihydroxy-, (7S,9S)-, hydrochloride (1:1) |(1S,3S)-3-acetyl-3,5,12-trihydroxy-6,11-dioxo-1,2,3,4,6,11-hexahydrotetracen-1-yl 3-amino-2,3,6-trideoxy-a-L-lyxo-hexopyranoside hydrochloride (1:1) |(7S-cis)-9-Acetyl-7-((3-amino-2,3,6-trideoxy-α-L-lyxo-hexopyranosyl)oxy)-7,8,9,10-tetrahydro-6,9,11-trihydroxynaphthacene-5,12-dione hydrochloride |(1S,3S)-3-Acetyl-3,5,12-trihydroxy-6,11-dioxo-1,2,3,4,6,11-hexahydrotetracen-1-yl 3-amino-2,3,6-trideoxy-α-L-lyxo-hexopyranoside hydrochloride (1:1) |Idamycin |5,12-naphthacenedione, 9-acetyl-7-[(3-amino-2,3,6-trideoxy-a-L-lyxo-hexopyranosyl)oxy]-7,8,9,10-tetrahydro-6,9,11-trihydroxy-, (7S,9S)-, hydrochloride (1:1) |Zavedos |(7S-cis)-9-Acetyl-7-((3-amino-2,3,6-trideoxy-a-L-lyxo-hexopyranosyl)oxy)-7,8,9,10-tetrahydro-6,9,11-trihydroxynaphthacene-5,12-dione Hydrochloride |(7S,9S)-9-acetyl-7-{[(2R,4S,5S,6S)-4-amino-5-hydroxy-6-methyltetrahydro-2H-pyran-2-yl]oxy}-6,9,11-trihydroxy-7,8,9,10-tetrahydrotetracene-5,12-dione hydrochloride |Idarubicin HCL for research |IDARUBICIN HYDROCHLORIDE |4-Demethoxydaunorubicin hydrochloride |(1S,3S)-3-acetyl-3,5,12-trihydroxy-6,11-dioxo-1,2,3,4,6,11-hexahydrotetracen-1-yl 3-amino-2,3,6-trideoxy-α-L-lyxo-hexopyranoside hydrochloride |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-

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

盐酸依达比星毒性和生态

盐酸依达比星毒性英文版

盐酸依达比星安全

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