Chlorhydrate de doxorubicine (chlorhydrate d'hydroxydaunorubicine), un antibiotique anthracycline cytotoxique, est un agent de chimiothérapie anticancéreuse. Chlorhydrate de doxorubicine inhibe la topoisomérase, arrêtant ainsi la réplication de l'ADN. Chlorhydrate de doxorubicine réduit la phosphorylation basale de AMPK et de son cible en aval acétyl-CoA carboxylase. Chlorhydrate de doxorubicine induit l'apoptose et l'autophagie.
Doxorubicin hydrochloride (Hydroxydaunorubicin hydrochloride), ein zytotoxisches Anthracyclin-Antibiotikum, ist ein Chemotherapeutikum gegen Krebs. Doxorubicinhydrochlorid hemmt die topoisomerase II und stoppt so die DNA-Replikation. Doxorubicin-Hydrochlorid reduziert die basale Phosphorylierung von AMPK und seiner nachgeschalteten Ziel-Acetyl-CoA-Carboxylase. Doxorubicinhydrochlorid induziert apoptosis und autophagy.
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.
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Doxorubicin hydrochloride Chemical Structure
CAS No. : 25316-40-9
This product is a controlled substance and not for sale in your territory.
Based on 433 publication(s) in Google Scholar
Other Forms of Doxorubicin hydrochloride:
Doxorubicin-13C,d3
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Doxorubicin
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Doxorubicin hydrochloride (Standard)
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Doxorubicin hydrochloride purchased from MedChemExpress. Usage Cited in:
Cell Death Dis. 2019 Nov 25;10(12):887.
[Abstract]
Doxorubicin or CPT-11 significantly promoted KRT8 expression in chordoma cells in vitro. Western blotting analysis and quantification of KRT8 protein expression (normalized to GAPDH expression).
Doxorubicin hydrochloride purchased from MedChemExpress. Usage Cited in:
Cell Death Dis. 2019 Nov 25;10(12):887.
[Abstract]
Doxorubicin or CPT-11 significantly promoted KRT8 expression in chordoma cells in vitro. Representative images of immunofluorescence staining of KRT8 of CM318 and UCH1 cell line.
Effects of YWPC (50 mg/L for 24 h) on DOX (5 μM for 24 h)-induces dissipation of mitochondrial membrane potential measured in H9C2 cells loaded with JC-1 using fluorescence microscopy.
Doxorubicin hydrochloride purchased from MedChemExpress. Usage Cited in:
Nat Commun. 2018 Oct 8;9(1):4139.
[Abstract]
One hour after treated with UV or 2 h after treated with MMS, Camptothecin (CPT) (10 μM), or Doxorubicin (DOX; 0.5 μM), HEK293T cells expressing HA-SUMO2 and His-RhoB are subjected to sumoylation assay to detect the SUMO2 conjugation of RhoB.
Doxorubicin hydrochloride purchased from MedChemExpress. Usage Cited in:
J Clin Invest. 2018 Jan 2;128(1):483-499.
[Abstract]
Immunoblotting for EZH2 in lysates of immortalized mouse podocytes after treatment with Adriamycin (300 ng/mL) for 48 hours (n=6).
Doxorubicin hydrochloride purchased from MedChemExpress. Usage Cited in:
J Exp Clin Cancer Res. 2018 Sep 19;37(1):232.
[Abstract]
Immunoblotting shows that both P-gp protein expression is significantly decreased in 24 h after US exposure in MCF-7/ADR and HEPG2/ADM cells.
Doxorubicin hydrochloride purchased from MedChemExpress. Usage Cited in:
Nanoscale Res Lett. 2018 Nov 3;13(1):350.
[Abstract]
HY-15142
Doxorubicin hydrochloride purchased from MedChemExpress. Usage Cited in:
Cell Signal. 2017 May 1;36:108-116.
[Abstract]
PAQR3 affects DNA damage repair. AGS cells are treated with different doses of VP-16 (for 24 h), CDDP (for 24 h) and Doxorubicin (for 10 h) as indicated, followed by immunoblotting with the antibodies.
U937 cells are treated with Thapsigargin (TG, 1 μM), NSC 125973 (PTX, 5nM) as well as Doxorubincin (DOX, 1 μM) for 12 hours and the indicated proteins are detected by Western blot.
Immunofluorescent staining for α-actinin (ACTN2) and cardiac troponin T (TNNT2) to demonstrate sarcomeric organization in hiPSC–CMs derived from patients who do not experience Doxorubicin–induced cardiotoxicity (DOX) versus those who do experience Doxorubicin-induced cardiotoxicity (DOXTOX) after 24 h treatment with Doxorubicin. Scale bar, 20 µm.
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Auristatin Calicheamicins Camptothecins Daunorubicins/Doxorubicins Duocarmycins Maytansinoids Pyrrolobenzodiazepines Traditional Cytotoxic Agents
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].
IC50 & Target[1][2][3]
Topoisomerase I
0.8 μM (IC50)
Topoisomerase II
2.67 μM (IC50)
Daunorubicins/Doxorubicins
HIV-1
In Vitro
Doxorubicin hydrochloride (1-8 μM; 24 and 48 hours) decreases the viability of MCF-10F, MCF-7 and MDA-MB-231 cells in a time- and dose-dependent manner[4].
Doxorubicin hydrochloride (1 μM; 3 and 24 hours) results in Hct-116 human colon carcinoma cells reduction in G0/G1 phase and accumulation in G2 phase[5].
Doxorubicin hydrochloride (1 μM for MCF-10F and MDA-MB-231 cells, 4 μM for MCF-7 cells; 48 hours) induces apoptosis by upregulating Bax, caspase-8 and caspase-3 and downregulation of Bcl-2 protein expression[4].
Doxorubicin hydrochloride (5 μM; 10-30 min) can be accumulated in B16-F10 melanoma cell line CRL-6475 in a time-dependent manner, and can be detected by green or red fluorescence (green fluorescence has higher detection sensitivity) with a maximum excitation wavelength (λex) and a maximum emission wavelength (λem) of 470 nm and 560 nm, respectively[8]. Note:Doxorubicin hydrochloride is suitable for neutral or weakly acidic solvents; PBS (PH 7.4) is not recommended for dissolution, which may affect the dissolution effect.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Doxorubicin hydrochloride Related Antibodies
Cell Viability Assay[4]
Cell Line:
Breast cancer cell lines MCF-10F, MCF-7 and MDA-MB-231
Concentration:
0, 1, 2, 4 and 8 μM
Incubation Time:
24 and 48 hours
Result:
IC50 was 1 μM for both MCF-10F and MDA-MB-231 cell lines.
IC50 was 4 μM for MCF-7 cell line.
Cell Cycle Analysis[5]
Cell Line:
Hct-116 human colon carcinoma cells
Concentration:
1 μM
Incubation Time:
3 hours and 24 hours
Result:
Both, bolus (3 h) and continuous (24 h) incubation led to a significant reduction of cells in G0/G1 and accumulation in G2 phase.
Western Blot Analysis[4]
Cell Line:
Breast cancer cell lines MCF-10F, MCF-7 and MDA-MB-231
Concentration:
1 μM for MCF-10F and MDA-MB-231 cells, 4 μM for MCF-7 cells
Incubation Time:
48 hours
Result:
Bax protein expression was upregulated in MCF-10F and MDA-MB-231 cell lines but MCF-7 cells did not show any significant increase.
Caspase-8 gene expression was upregulated in MCF-10F, but it was downregulated in MCF-7 and MDA-MB-231 cells.
In Vivo
Doxorubicin hydrochloride can be used to induce models of cardiotoxicity and heart failure.
1. Inducing cardiotoxicity[10][11]
Background
The mechanism of short-term induction of cardiotoxicity: promoting extracellular remodeling of myocardium to induce heart failure, and also works at the molecular level. Including: interacting with iron, changing the activity of oxidases in cells or mitochondria, and binding to topoisomerases.
Specific Mmodeling Methods
Mice: Female C57BL/6j mice • 20-22 g • 6 weeks old Administration: 2 mg/kg, 10 mg/kg • ip • once every the other day for 2 or 3 times
Note
Mice were sacrificed 3 days after the first injection.
Modeling Indicators
molecular level: (1) Pro-inflammatory cytokines (such as TNF-α and IL-6) increase significantly, while anti-inflammatory cytokine IL-10 decreases; (2) Inducible - Nitric oxide synthase (iNOS) was overexpressed and serum nitrite levels were elevated; nitrotyrosine expression was significantly increased.
Correlated Product(s): /
Opposite Product(s): /
2. Induction of heart failure[11][12]
Background
The long-term mechanisms inducing heart failure remain to be carefully elucidated.
Specific Mmodeling Methods
Rat: Male Wistar rats • 180-200 g Administration: 2.5 mg/kg • ip • once every week, for 6 weeks • treated at 4 weeks later.
Note
Modeling Indicators
Cellular/tissue level: Myocardial sarcomeres are destroyed, mitochondria are swollen and damaged,
Myocardial cells showed inflammation and apoptosis (transmission electron microscopy results); myocardial fibrosis, and left ventricular collagen I and II levels were downregulated (immunohistochemistry results). Changes in macroscopic indicators: Hemodynamic parameters and echocardiography show cardiac insufficiency and impaired left ventricular function; such as increases in LVIDd, LVIDs and LVEDP.
Correlated Product(s): /
Opposite Product(s): Captopril (HY-B0368)
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Model:
Female MF1 nu/nu mice bearing MDA-G8 breast tumor xenograft (6-week-old)[6]
Moderate inhibition of subcutaneous tumor growth in mice that were treated with 2 mg/kg Doxorubicin alone or with 100 μg/kg Zoledronic acid alone compared to the saline control.
Mice treated with Zoledronic acid and Doxorubicin together had statistically significant smaller mean tumor volumes on day 42 than those treated with Doxorubicin alone.
Animal Model:
Male Sprague-Dawley rats[7]
Dosage:
1%, 2%, 4%, 5%, 6%, 10%, 20%
Administration:
Intrastriatal injection; Single dose
Result:
In doses of 4, 5, 6, 10 or 20% caused obvious loss of ipsilateral SNc and VTA neuronsz and doses of 1 or 2% failed to produce obvious neuron loss.
Room temperature in continental US; may vary elsewhere.
Storage
4°C, sealed storage, away from moisture and light
*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)
Solvent & Solubility
In Vitro:
H2O : 50 mg/mL (86.21 mM; ultrasonic and warming and heat to 60°C)
DMSO : 25 mg/mL (43.10 mM; ultrasonic and warming and heat to 60°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Preparing Stock Solutions
ConcentrationSolventMass
1 mg
5 mg
10 mg
1 mM
1.7242 mL
8.6210 mL
17.2420 mL
5 mM
0.3448 mL
1.7242 mL
3.4484 mL
10 mM
0.1724 mL
0.8621 mL
1.7242 mL
View the Complete Stock Solution Preparation Table
*Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles. Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
*
Note: If you choose water as the stock solution, please dilute it to the working solution,
then filter and sterilize it with a 0.22 μm filter before use.
For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day. The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μLDMSO stock solution (20.8 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Protocol 3
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μLDMSO stock solution (20.8 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
For the following dissolution methods, please prepare the working solution directly.
It is recommended to prepare fresh solutions and use them promptly within a short period of time. The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution.
If precipitation or phase separation occurs during preparation,
heat and/or sonication can be used to aid dissolution.
Protocol 1
Add each solvent one by one: Saline
Solubility: 8.33 mg/mL (14.36 mM); Clear solution; Need ultrasonic and warming and heat to 60°C
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:
Dosage
mg/kg
Animal weight (per animal)
g
Dosing volume (per animal)
μL
Number of animals
Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Calculation results:
Working solution concentration:
mg/mL
This product has good water solubility, please refer to the measured solubility data in water/PBS/Saline for details.
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only.If necessary, please contact MedChemExpress (MCE).
[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.
[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.
Complete Stock Solution Preparation Table
*Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles. Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Optional Solvent
ConcentrationSolventMass
1 mg
5 mg
10 mg
25 mg
DMSO / H2O
1 mM
1.7242 mL
8.6210 mL
17.2420 mL
43.1049 mL
5 mM
0.3448 mL
1.7242 mL
3.4484 mL
8.6210 mL
10 mM
0.1724 mL
0.8621 mL
1.7242 mL
4.3105 mL
15 mM
0.1149 mL
0.5747 mL
1.1495 mL
2.8737 mL
20 mM
0.0862 mL
0.4310 mL
0.8621 mL
2.1552 mL
25 mM
0.0690 mL
0.3448 mL
0.6897 mL
1.7242 mL
30 mM
0.0575 mL
0.2874 mL
0.5747 mL
1.4368 mL
40 mM
0.0431 mL
0.2155 mL
0.4310 mL
1.0776 mL
H2O
50 mM
0.0345 mL
0.1724 mL
0.3448 mL
0.8621 mL
60 mM
0.0287 mL
0.1437 mL
0.2874 mL
0.7184 mL
80 mM
0.0216 mL
0.1078 mL
0.2155 mL
0.5388 mL
*
Note: If you choose water as the stock solution, please dilute it to the working solution,
then filter and sterilize it with a 0.22 μm filter before use.
Doxorubicin hydrochloride Related Classifications
Induced Disease Models Products
Immunology and Inflammatory Disease ModelsCardiovascular System Disease ModelsUrinary System Disease Models
Nephritis ModelsHeart Disease Models
InfectionCancer
Cancer Targeted TherapyCancer ImmunotherapyCancer Metabolism and Metastasis
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.
Keywords:
Doxorubicin25316-40-9Hydroxydaunorubicin ADRTopoisomeraseADC CytotoxinAMPKAutophagyApoptosisHIVHBVMitophagyAntibioticBacterialADC PayloadAMP-activated protein kinaseHuman immunodeficiency virusHepatitis B virusMitochondrial AutophagyCardiotoxicityNeurotoxicityfluorescenceHelaCRL-6475fluorescence detectionantibioticstumorapoptosisautophagyInhibitorinhibitorinhibit
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