盐酸依达比星

• 常用名: 盐酸依达比星
• 英文名: Idarubicin (hydrochloride)
• 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
• 闪点: 392.5ºC
• 符号: GHS06, GHS08
• 信号词: Danger

盐酸依达比星用途

盐酸依达比星为蒽环类抗生素，有抗有丝分裂和细胞毒作用。盐酸依达比星作用机制为作用于拓扑异构酶II，抑制核酸全盛。蒽环结构4位的改变使该化合物具有新脂性，提高了细胞对经物的摄入。

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

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
• 靶点实验:

  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
• InChIKey: JVHPTYWUBOQMBP-RVFAQHLVSA-N
• SMILES: CC(=O)C1(O)Cc2c(O)c3c(c(O)c2C(OC2CC(N)C(O)C(C)O2)C1)C(=O)c1ccccc1C3=O.Cl
• 外观性状: 粉末
• 储存条件: -20℃

盐酸依达比星毒性和生态

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

盐酸依达比星靶点实验

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盐酸依达比星英文别名

• (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)