生物活性

• 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
• Cell Data

  Cell Lines	Concentration	Assay Type	Time	Activity Description	Data Sources
  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

• 更多
• 临床研究

• NCT号	适应症或疾病	临床期	招募状态	预计完成时间	地点
  NCT01698879	Novo Acute Myeloid Leukemia	Phase 2	Unknown	December 2016	Spain ... more >> Hospital Germans Trias i Pujol Badalona, Barcelona, Spain, 08916 Hospital de la Santa Creu i Sant Pau Barcelona, Spain, 08025 Hospital Clinic Barcelona Barcelona, Spain, 08036 Hospital Clinico Universitario de Salamanca Salamanca, Spain, 37007 Hospital Universitario Virgen del Rocio Sevilla, Spain, 41013 Hospital Clínico Universitario de Valencia Valencia, Spain, 496010 Collapse <<
  NCT02671708	Autologous Hematopoietic Stem ... more >>Cell Transplantation Acute Myeloid Leukemia Conditioning Collapse <<	Phase 2 Phase 3	Recruiting	December 2019	China, Guangdong ... more >> Department of Hematology,Nanfang Hospital, Southern Medical University Recruiting Guangzhou, Guangdong, China, 510515 Contact: Li Xuan    +86-020-61641613    356135708@qq.com    Principal Investigator: Qifa Liu Collapse <<
  NCT01067274	Acute Myeloid Leukemia	Phase 3	Withdrawn(Study abandoned)	-	France ... more >> Chu Amiens Sud Amiens, France, 80054 CH Argenteuil, France, 95107 Hopital Avicenne Bobigny, France Chu Boulogne Sur Mer Boulogne Sur Mer, France, 62321 CH Caen, France, 14033 Hopital Percy Clamart, France, 92141 Ch Sud Francilien Corbeil Essonnes, France, 94010 Hopital Henri Mondor Creteil, France Ch Dunkerque Dunkerque, France, 59385 CH Lens, France, 62307 CHU Lille, France, 59037 CH Limoges, France, 87042 Hopital Edouard Herriot Lyon, France CH Meaux, France, 77104 Centre Antoine Lacassagne Nice, France, 06189 Necker Hospital Paris 15, France, 75015 St Antoine Hospital Paris, France, 75012 Hopital Pitie-Salpetriere Paris, France, 75651 Hopital Saint-Louis Paris, France Ch Rene Dubos Pontoise, France, 95303 CH Roubaix, France, 59100 CHU Rouen, France, 76038 CNLCC Saint-Cloud, France, 92210 CH Valenciennes, France, 59322 CH Versailles, France IGR Villejuif, France Collapse <<

• 更多
• 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.

• 更多

• Collapse