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MCE 国际站：Doxorubicin (hydrochloride)
中文名：盐酸阿霉素
CAS：25316-40-9
品牌：MedChemExpress (MCE)
存储条件：4°C, sealed storage, away from moisture and light
生物活性：Doxorubicin (Hydroxydaunorubicin) hydrochloride 是一种细胞毒性蒽环类抗生素，是一种抗癌化疗药物。 Doxorubicin hydrochloride 是一种有效的人类 DNA 拓扑异构酶 I 和 拓扑异构酶 II 抑制剂，IC50 分别为 0.8 μM 和 2.67 μM，分别。 Doxorubicin hydrochloride 降低 AMPK 及其下游靶标乙酰辅酶 A 羧化酶的基础磷酸化。 Doxorubicin hydrochloride 诱导细胞凋亡和自噬[1][2][3]。 IC50 和目标：IC50：0.8 μM（拓扑异构酶 I）[3]，2.67 μM（拓扑异构酶 II）[1]
体外：盐酸多柔比星（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] .
阿霉素盐酸盐（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]。
盐酸多柔比星（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< sup>[4].
体内：与生理盐水相比，单独使用多柔比星 (2 mg/kg) 或唑来膦酸 (100 μg/kg) 治疗不会显着降低最终肿瘤体积。接受多柔比星加唑来膦酸治疗的小鼠的最终肿瘤体积明显小于仅接受多柔比星治疗的小鼠[6]。
热销产品：Tofacitinib | Dabrafenib | Stigmastanol | O-Propargyl-Puromycin | JC-1 | Conduritol B epoxide | Tocilizumab | Rituximab | Secukinumab | sulfo-SPDB-DM4
研究领域：Cell Cycle/DNA Damage | Antibody-drug Conjugate/ADC Related | Epigenetics | PI3K/Akt/mTOR | Autophagy | Apoptosis | Anti-infection
作用靶点：Topoisomerase | ADC Cytotoxin | AMPK | Autophagy | Apoptosis | HIV | HBV | Mitophagy | Antibiotic | Bacterial
Trending products：Recombinant Proteins | Bioactive Screening Libraries | Natural Products | Fluorescent Dye | PROTAC | Isotope-Labeled Compounds | Oligonucleotides
参考文献：
[1]. John L. Nitiss, et al. Targeting DNA topoisomerase II in cancer chemotherapy.Nat Rev Cancer. 2009 May;9(5):338-50.
[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.
[3]. P D Foglesong, et al. Doxorubicin inhibits human DNA topoisomerase I. Cancer Chemother Pharmacol. 1992;30(2):123-5.
[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.
[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.
[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.
[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
[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.
[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.
