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Idarubicin HCl

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Chemical Structure| 57852-57-0 同义名 : 伊达比星盐酸盐 ;4-Demethoxydaunorubicin hydrochloride;Idarubicin (hydrochloride);NSC 256439;4-DMD;4-Demethoxydaunorubicin;4-demethoxydaunorubicin HCl;Idarubicin hydrochloride
CAS号 : 57852-57-0
货号 : A131979
分子式 : C26H28ClNO9
纯度 : 99%+
分子量 : 533.955
MDL号 : MFCD00897212
存储条件:

粉末 Inert atmosphere,2-8°C

液体 -20°C:3-6个月-80°C:12个月

溶解度 :

DMSO: 85 mg/mL(159.19 mM),配合低频超声助溶,注意:DMSO长时间开封后,会吸水并导致溶解能力下降,请避免使用长期开封的DMSO

动物实验配方:
生物活性
靶点
  • Topo II

    Topo II (MCF-7 cells), IC50:3.3 ng/mL

描述 Idarubicin is a 4-demethoxy analog of the leukemia therapeutic daunorubicin, which intercalate in DNA and inhibit topoisomerase II, resulting in cancer cell cytotoxicity at lo concentration (IC50=20-120nM)[3]. Idarubicin has shown a greater cytotoxicity than daunorubicin or doxorubicin in various in vitro systems. This has been attributed to a better ability of idarubicin to induce the formation of topoisomerase II -mediated DNA breaks[4]. Idarubicin produces a concentration-dependent reduction in cell growth, with an IC50 value of approximately 0.01 μM. Idarubicin produced a concentration-dependent inhibition of DNA synthesis[5].
细胞研究
细胞系 浓度 检测类型 检测时间 活动说明 数据源
HepG2 cells Function assay Inhibition of liver stage Plasmodium berghei infection in HepG2 cells, IC50=6.62 μM 22586124
human ES2 cells Cytotoxic assay 24 h Cytotoxicity against human ES2 cells after 24 hrs by XTT assay, IC50=3.2 μM 24900668
human K562 cells Proliferation assay 72 h Antiproliferative activity against human K562 cells after 72 hrs, GI50=3.3 μM 25420175
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

1.87mL

0.37mL

0.19mL

9.36mL

1.87mL

0.94mL

18.73mL

3.75mL

1.87mL

参考文献

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

[2]Colburn DE, Giles FJ, et al. In vitro evaluation of cytochrome P450-mediated drug interactions between cytarabine, idarubicin, itraconazole and caspofungin. Hematology. 2004 Jun;9(3):217-21.

[3]Dautant A, Langlois d'Estaintot B, Gallois B, Brown T, Hunter WN. A trigonal form of the idarubicin:d(CGATCG) complex; crystal and molecular structure at 2.0 A resolution. Nucleic Acids Res. 1995 May 25;23(10):1710-6.

[4]Robert J. Clinical pharmacokinetics of idarubicin [published correction appears in Clin Pharmacokinet 1993 Oct;25(4):350]. Clin Pharmacokinet. 1993;24(4):275-288.

[5]Gewirtz DA, Randolph JK, Chawla J, Orr MS, Fornari FA. 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):361-369.