Doxorubicin
mRNA synthesis
In vitro transcription of capped mRNA with modified nucleotides and Poly(A) tail
Tyramide Signal Amplification (TSA)
TSA (Tyramide Signal Amplification), used for signal amplification of ISH, IHC and IC etc.
Phos Binding Reagent Acrylamide
Separation of phosphorylated and non-phosphorylated proteins without phospho-specific antibody
Cell Counting Kit-8 (CCK-8)
A convenient and sensitive way for cell proliferation assay and cytotoxicity assay
SYBR Safe DNA Gel Stain
Safe and sensitive stain for visualization of DNA or RNA in agarose or acrylamide gels.
Inhibitor Cocktails
Protect the integrity of proteins from multiple proteases and phosphatases for different applications.
Doxorubicin（多柔比星）是从细菌培养物中分离的半合成抗癌剂[1]，是一种蒽环类抗生素，被广泛用于血液癌症、实体瘤和肉瘤。
Doxorubicin插入DNA双链中，抑制DNA拓扑异构酶II的运动，停止复制过程[2]。Doxorubicin也诱导组蛋白从开放的染色质中驱逐，引起DNA损伤和表观遗传失调[3]。
Doxorubicin通过静脉给药。将近75%的doxorubicin及其代谢物与血浆蛋白结合。Doxorubicin不能穿过血脑屏障。50％的药物主要通过胆汁排泄从身体中消除，剩下的药物经过单电子还原、二电子还原和去糖苷化，其主要代谢物是一种有效的膜离子泵抑制剂，与心肌病相关[4]。
参考文献：
[1]Brayfield, A, ed. (2013). Doxorubicin. Martindale: The Complete Drug Reference. Pharmaceutical Press. Retrieved 15 April 2014.
[2]Pommier Y. , et al. (2010). DNA topoisomerases and their poisoning by anticancer and antibacterial drugs. Chemistry & Biology 17 (5): 421–433.
[3]Pang, B. , et al. (2013). Drug-induced histone eviction from open chromatin contributes to the chemotherapeutic effects of doxorubicin. Nature Communications 4 (5): 1908
[4]Boucek RJ. , et al. (1987). The major metabolite of doxorubicin is a potent inhibitor of membrane-associated ion pumps. A correlative study of cardiac muscle with isolated membrane fractions. J of Biol Chem 262: 15851-15856.
- 1. Riley Plett, Paul Mellor, et al. "Homoharringtonine demonstrates a cytotoxic effect against triple-negative breast cancer cell lines and acts synergistically with paclitaxel." Sci Rep. 2022 Sep 19;12(1):15663. PMID: 36123435
- 2. Ji Yun Lee, Joo Hyun Kim, et al. "EGR1 as a potential marker of prognosis in extranodal NK/T-cell lymphoma." Sci Rep. 2021 May 14;11(1):10342. PMID: 33990633
- 3. Zhongying Gong, Xiaoying Liu, et al. "Tumor acidic microenvironment-induced drug release of RGD peptide nanoparticles for cellular uptake and cancer therapy." Colloids Surf B Biointerfaces. 2021 Mar 4;202:111673. PMID: 33714186
- 4. Ji Yun Lee, Joo Hyun Kim, et al. "Gene Expression Profiling in Extranodal NK/T-Cell Lymphoma." Research Square. December 4th, 2020.
- 5. Wang X, Wang Q, et al. "TFEB-NF-κB inflammatory signaling axis: a novel therapeutic pathway of Dihydrotanshinone I in doxorubicin-induced cardiotoxicity." J Exp Clin Cancer Res. 2020;39(1):93. PMID: 32448281
- 6. Gong Z, Lao J, et al. "pH-Triggered geometrical shape switching of a cationic peptide nanoparticle for cellular uptake and drug delivery." Colloids Surf B Biointerfaces. 2020;188:110811. PMID: 31982793
- 7. Qi W, Boliang W, et al. "Cardamonin protects against doxorubicin-induced cardiotoxicity in mice by restraining oxidative stress and inflammation associated with Nrf2 signaling." Biomed Pharmacother. 2020;122:109547. PMID: 31918264
- 8. Gong Z, Shi Y, et al. "Plasma Amine Oxidase-Induced Nanoparticle-to-Nanofiber Geometric Transformation of an Amphiphilic Peptide for Drug Encapsulation and Enhanced Bactericidal Activity." ACS Appl Mater Interfaces. 2020;12(4):4323–4332. PMID: 31899611
- 9. Gong Z, Liu X, Wu J, et al. "pH-triggered morphological change in a self-assembling amphiphilic peptide used as an antitumor drug carrier." Nanotechnology. 2020;31(16):165601. PMID: 31891937
- 10. Yan L, Ding B, et al. "Inhibition of SMYD2 suppresses tumor progression by down-regulating microRNA-125b and attenuates multi-drug resistance in renal cell carcinoma." Theranostics. 2019 Oct 22;9(26):8377-8391. PMID: 31754403
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- 12. Wang X, Li C, et al. "Tanshinone IIA Restores Dynamic Balance of Autophagosome/Autolysosome in Doxorubicin-Induced Cardiotoxicity via Targeting Beclin1/LAMP1." Cancers (Basel). 2019 Jun 28;11(7). pii: E910. PMID: 31261758
- 13. Zhang Y, Xia F, et al. "miR-135b-5p enhances doxorubicin-sensitivity of breast cancer cells through targeting anterior gradient 2." J Exp Clin Cancer Res. 2019 Jan 21;38(1):26. PMID: 30665445
- 14. Goodspeed A, Jean A, et al. "A Whole-genome CRISPR Screen Identifies a Role of MSH2 in Cisplatin-mediated Cell Death in Muscle-invasive Bladder Cancer." Eur Urol. 2019 Feb;75(2):242-250. PMID: 30414698
- 15. Deng Y, Li F, et al. "Triptolide sensitizes breast cancer cells to Doxorubicin through the DNA damage response inhibition." Mol Carcinog. 2018 Jun;57(6):807-814. PMID: 29500880
| Physical Appearance | A solid |
| Storage | Powder: Store at RT; Solution: Store at -20°C |
| M.Wt | 543.52 |
| Cas No. | 23214-92-8 |
| Formula | C27H29NO11 |
| Synonyms | Adriamycin, Doxil, Adriablastin, Doxorubicinum, Myocet |
| Solubility | ≥27.2 mg/mL in DMSO; insoluble in EtOH; ≥24.8 mg/mL in H2O with ultrasonic |
| Chemical Name | (7S,9S)-7-[(2R,4S,5S,6S)-4-amino-5-hydroxy-6-methyloxan-2-yl]oxy-6,9,11-trihydroxy-9-(2-hydroxyacetyl)-4-methoxy-8,10-dihydro-7H-tetracene-5,12-dione |
| SDF | Download SDF |
| Canonical SMILES | CC1C(C(CC(O1)OC2CC(CC3=C(C4=C(C(=C23)O)C(=O)C5=C(C4=O)C=CC=C5OC)O)(C(=O)CO)O)N)O |
| 运输条件 | 蓝冰运输或根据您的需求运输。 |
| 一般建议 | 不同厂家不同批次产品溶解度各有差异，仅做参考。若实验所需浓度过大至产品溶解极限，请添加助溶剂助溶或自行调整浓度。溶液形式一般不宜长期储存，请尽快用完。 |
| 细胞实验 [1]: | |
|
细胞系 |
MDA-MB-231细胞 |
|
制备方法 |
可溶于DMSO。若配制更高浓度的溶液，一般步骤如下：请将试管置于37℃加热10分钟和/或将其置于超声波浴中震荡一段时间。原液于-20℃可放置数月。 |
|
反应条件 |
20 nM；72小时 |
|
实验结果 |
在MDA-MB-231细胞中，SH003 (120 μg/mL) 和Doxorubicin (20 nM) 联合使用具有协同作用。 |
| 动物实验 [2]: | |
|
动物模型 |
皮下注射MB231细胞的雌性无胸腺裸鼠 |
|
给药剂量 |
3 mg/kg/day；瘤内给药 |
|
实验结果 |
Doxorubicin与腺病毒MnSOD (AdMnSOD) 以及1,3-双（2-氯乙基）-1-亚硝基脲 (BCNU) 联合用药有效降低MB231肿瘤体积并延长小鼠生存期。 |
|
其它注意事项 |
请于室内测试所有化合物的溶解度。虽然化合物的实际溶解度可能与其理论值略有不同，但仍处于实验系统误差的允许范围内。 |
|
References: [1]. Woo SM, Kim AJ, Choi YK, Shin YC, Cho SG, Ko SG. Synergistic Effect of SH003 and Doxorubicin in Triple-negative Breast Cancer. Phytother Res. 2016 Aug 1. [2]. Sun W, Kalen AL, Smith BJ, Cullen JJ, Oberley LW. Enhancing the antitumor activity of adriamycin and ionizing radiation. Cancer Res. 2009 May 15;69(10):4294-300. |
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| 描述 | Doxorubicin（Adriamycin）是一种抗生素，DNA拓扑异构酶II的抑制剂，DNA损伤和细胞凋亡的诱导剂。 | |||||
| 靶点 | Autophagy | |||||
| IC50 | ||||||
质量控制和MSDS
- 批次:
化学结构
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