Doxorubicin (Adriamycin) HCl
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是从细菌培养得到的半合成抗癌药 [1]。它是一种蒽环类抗生素,被广泛地应用于血癌,实体瘤和肉瘤。
Doxorubicin嵌入到DNA双链,抑制DNA拓扑异构酶II的前行,停止复制过程 [2]。Doxorubicin也能从开放的染色质上驱逐组蛋白,引起DNA损伤和减弱对表观遗传的控制 [3]。
Doxorubicin通过静脉给药,约75%的Doxorubicin及其代谢物与血浆蛋白结合。Doxorubicin不能跨越血脑屏障。50%的药物保持原型被排出体外,主要通过胆汁排泄途径。剩余的部分参与单电子还原、双电子还原和去糖苷化反应。主要代谢物是一种与心肌病相关的高效膜离子泵抑制剂[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. Xinxing Ye, Jie Zhou, et al. "E2F1 Affects the Therapeutic Response to Neoadjuvant Therapy in Breast Cancer." Dis Markers. 2022 Sep 17;2022:8168517. PMID: 36164372
- 2. Sarkar R, Patra U, et al. "Rotavirus activates a noncanonical ATM-Chk2 branch of DNA damage response during infection to positively regulate viroplasm dynamics." Cell Microbiol. 2019 Dec 17:e13149. PMID: 31845505
- 3. Kai Wang, Jing Dai, et al. "LncRNA ZEB2-AS1 regulates the drug resistance of acute myeloid leukemia via the miR-142-3p/INPP4B axis." RSC Adv., 2019, 9, 39495-39504.
- 4. Lin KH, Xie A, et al. "Systematic Dissection of the Metabolic-Apoptotic Interface in AML Reveals Heme Biosynthesis to Be a Regulator of Drug Sensitivity." Cell Metab. 2019 Feb 5. pii: S1550-4131(19)30011-7. PMID: 30773463
- 5. Andrew Goodspeed, Annie Jean, et al. "Low MSH2 protein levels identify muscle-invasive bladder cancer resistant to cisplatin." bioRxiv. 2018 June 29.
Physical Appearance | A solid |
Storage | Store at -20°C |
M.Wt | 579.98 |
Cas No. | 25316-40-9 |
Formula | C27H29NO11·HCl |
Solubility | ≥29 mg/mL in DMSO; ≥57.2 mg/mL in H2O; insoluble in EtOH |
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;hydrochloride |
SDF | Download SDF |
Canonical SMILES | COC1=C2C(C(C3=C(C2=O)C(O)=C4C(C[C@](O)(C[C@@H]4O[C@@]5([H])C[C@@H]([C@@H]([C@@H](O5)C)O)N)C(CO)=O)=C3O)=O)=CC=C1.Cl |
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 |
H9c2 细胞 |
溶解方法 |
该化合物在DMSO中的溶解度大于10 mM。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 |
1 μg/ml, 2 小时 |
实验结果 |
使用逐渐增加浓度的doxorubicin处理H9c2细胞2小时,浓度为0.1、0.3、0.5和1.0 μg/ml,分别相当于0.17、0.52、0.85和1.71 μM,或使用0.3 μg/ml(相当于0.52μM)的doxorubicin处理不同时间。Doxorubicin以时间和剂量依赖性的方式诱导AMPKα(Thr 172)及其下游乙酰辅酶A羧化酶(ACC,Ser 79)的磷酸化。Doxorubicin处理1小时后,AMPKα的磷酸化较为显著,药物效果维持至少6小时。LKB1可能是AMPK的上游激酶,在H9c2细胞中,Doxorubicin也激活LKB1。 |
动物实验 [2]: | |
动物模型 |
C57BL/10 小鼠 |
剂量 |
腹膜内注射,20 mg/kg |
实验结果 |
与对照组相比,doxorubicin注射后5天,小鼠的收缩期 (LVP, -29%; dP/dtmax, -45%)、舒张期(dP/dtmin, -44%; stiffness, +275%) 以及全局左心室(LV)功能 (SV, -61%; HR, -18%; CO,-68%) 显著受损。与安慰剂小鼠相比,心脏脂质过氧化活性(+37%)和心脏硝基酪氨酸蛋白表达(+204%)均有所增加。 |
注意事项 |
请测试所有化合物在室内的溶解度,实际溶解度和理论值可能略有不同。这是由实验系统的误差引起的,属于正常现象。 |
References: [1] Chen M B, Wu X Y, Gu J H, et al. Activation of AMP-activated protein kinase contributes to doxorubicin-induced cell death and apoptosis in cultured myocardial H9c2 cells. Cell biochemistry and biophysics, 2011, 60(3): 311-322. [2] Riad A, Bien S, Westermann D, et al. Pretreatment with statin attenuates the cardiotoxicity of Doxorubicin in mice. Cancer research, 2009, 69(2): 695-699. |
描述 | Doxorubicin是一种抗肿瘤抗生素,对DNA拓扑异构酶Ⅱ具有抑制作用。 | |||||
靶点 | MCF-7 | |||||
IC50 | 100 nM |
质量控制和MSDS
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