Doxorubicin 是一种有细胞毒性的蒽环类抗生素，用于治疗多种癌症。 Doxorubicin 在癌细胞中起作用的可能机制是嵌入 DNA 和破坏 topoisomerase-II 介导的DNA修复。

Doxorubicin (Hydroxydaunorubicin) hydrochloride, a cytotoxic anthracycline antibiotic, is an anti-cancer chemotherapy agent. Doxorubicin hydrochloride is a potent human DNA topoisomerase I and topoisomerase II inhibitor with IC50s of 0.8 μM and 2.67 μM, respectively. Doxorubicin hydrochloride reduces basal phosphorylation of AMPK and its downstream target acetyl-CoA carboxylase. Doxorubicin hydrochloride induces apoptosis and autophagy[1][2][3].

固体

Doxorubicin hydrochloride (1-8 μM；24 和 48 小时) 以时间和剂量依赖性方式降低 MCF-10F、MCF-7 和 MDA-MB-231 细胞的活力[4]。
Doxorubicin hydrochloride (1 μM；3 和 24 小时) 导致 Hct-116 人结肠癌细胞在 G0/G1 期减少和在 G2 期积累[5]。
Doxorubicin hydrochloride (MCF-10F 和 MDA-MB-231 细胞为 1 μM，MCF-7 细胞为 4 μM；48 小时) 通过上调 Bax、caspase-8 和 caspase-3 以及下调 Bcl-2 蛋白表达诱导细胞凋亡[4]。
Doxorubicin hydrochloride (5 μM; 10-30 分钟) 在 B16-F10 黑色素瘤细胞系 CRL-6475 细胞中能以时间依赖方式在细胞中积累，且可以通过绿色或红色荧光来进行检测 (绿色荧光的检测灵敏度更高), 最大激发波长 (λex) 和最大发射波长 (λem) 分别为 470 nm 和 560 nm[8]。
注意：
Doxorubicin hydrochloride 适合中性或者弱酸性的溶剂，不建议使用 PBS (PH 7.4) 进行溶解，可能会影响溶解效果。

Room temperature in continental US; may vary elsewhere.

4°C, sealed storage, away from moisture and light

Quinones Anthraquinones

[1]. John L. Nitiss, et al. Targeting DNA topoisomerase II in cancer chemotherapy.Nat Rev Cancer. 2009 May;9(5):338-50.  [Content Brief]

[2]. Hee-KyungRhee,et al. Synthesis, cytotoxicity, and DNA topoisomerase II inhibitory activity of benzofuroquinolinediones. Bioorg Med Chem. 2007 Feb 15;15(4):1651-8.  [Content Brief]

[3]. P D Foglesong, et al. Doxorubicin inhibits human DNA topoisomerase I. Cancer Chemother Pharmacol. 1992;30(2):123-5.  [Content Brief]

[4]. Nesstor Pilco-Ferreto, et al. Influence of doxorubicin on apoptosis and oxidative stress in breast cancer cell lines. Int J Oncol. 2016 Aug;49(2):753-62.  [Content Brief]

[5]. Regine Lüpertz, et al. Dose- and time-dependent effects of doxorubicin on cytotoxicity, cell cycle and apoptotic cell death in human colon cancer cells. Toxicology. 2010 May 27;271(3):115-21.  [Content Brief]

[6]. Penelope D Ottewell, et al. Antitumor effects of doxorubicin followed by zoledronic acid in a mouse model of breast cancer. J Natl Cancer Inst. 2008 Aug 20;100(16):1167-78.  [Content Brief]

[7]. Koda LY, Van der Kooy D. Doxorubicin: a fluorescent neurotoxin retrogradely transported in the central nervous system. Neurosci Lett. 1983 Mar 28;36(1):1-8. doi: 10.1016/0304-3940(83)90476-7. PMID: 6190113. 9  [Content Brief]

[8]. Kauffman MK, Kauffman ME, Zhu H, Jia Z, Li YR. Fluorescence-Based Assays for Measuring Doxorubicin in Biological Systems. React Oxyg Species (Apex). 2016;2(6):432-439. doi: 10.20455/ros.2016.873. PMID: 29707647; PMCID: PMC5921830.  [Content Brief]

[9]. Mirza A Z, Shamshad H. Preparation and characterization of doxorubicin functionalized gold nanoparticles[J]. European journal of medicinal chemistry, 2011, 46(5): 1857-1860.