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  4. Doxorubicin hydrochloride

Doxorubicin hydrochloride  (Synonyms: Hydroxydaunorubicin hydrochloride)

Cat. No.: HY-15142 Purity: 99.90%
COA Handling Instructions

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.

For research use only. We do not sell to patients.

Doxorubicin hydrochloride Chemical Structure

Doxorubicin hydrochloride Chemical Structure

CAS No. : 25316-40-9

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Customer Review

Based on 395 publication(s) in Google Scholar

Other Forms of Doxorubicin hydrochloride:

Top Publications Citing Use of Products

384 Publications Citing Use of MCE Doxorubicin hydrochloride

WB
IF
IHC

    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.

    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: Free Radic Biol Med. 2019 Jan;130:557-567.  [Abstract]

    Representative pictures of Live/Dead staining of effects of 7,8-DHF on high dose of Dox-induced cell death and MMP reduction of H9c2 cells.

    Doxorubicin hydrochloride purchased from MedChemExpress. Usage Cited in: J Cell Mol Med. 2019 Sep;23(9):6034-6047.  [Abstract]

    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.

    Doxorubicin hydrochloride purchased from MedChemExpress. Usage Cited in: Cell Physiol Biochem. 2017;42(3):965-973.  [Abstract]

    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.

    Doxorubicin hydrochloride purchased from MedChemExpress. Usage Cited in: Nat Med. 2016 May;22(5):547-56.  [Abstract]

    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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    • Biological Activity

    • Purity & Documentation

    • References

    • Customer Review

    Description

    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 can label neuron cells, and it is bright red under Rhodamine filter bag, and light red-orange under catecholamine filter bag[7].
    Doxorubicin (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 wavelengthex) and a maximum emission wavelengthem) 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.

    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 (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 can label neuron cells, and it is bright red under Rhodamine filter bag, and light red-orange under catecholamine filter bag[7].
    Doxorubicin (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 wavelengthex) and a maximum emission wavelengthem) 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.

    Doxorubicin hydrochloride can be used in animal modeling to construct animal heart failure models. Treatment with Doxorubicin (2 mg/kg) or Zoledronic acid (100 μg/kg) alone does not statistically significantly decrease final tumor volume compared with saline. Mice treated with Doxorubicin plus Zoledronic acid have statistically significantly smaller final tumor volumes than those treated with Doxorubicin alone[6]. Doxorubicin (4%-20%; Intrastriatal injection; Single dose) is neurotoxic in Sprague-Dawley mice[7].
    Doxorubicin can be coupled to gold nanoparticles (Au NPs) by PH-sensitive bonding under acidic conditions, allowing it to pass through the blood-brain barrier with a maximum absorption wavelength of 528 nm[9].

    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 Modeling 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 • Sacrificed mouse in 3 days after the first injection.
    Note
    Modeling Indicators
    Changes at the 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.

    2. Induction of heart failure[11][12]
    Background
    The long-term mechanisms inducing heart failure remain to be carefully elucidated.
    Specific Modeling 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]
    Dosage: Doxorubicin (2 mg/kg); Zoledronic acid (100 μg/kg)
    Administration: Intravenous injection; once a week; 6 weeks
    Result: 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.
    Clinical Trial
    Molecular Weight

    579.98

    Formula

    C27H30ClNO11

    CAS No.
    Appearance

    Solid

    Color

    Red to orange

    SMILES

    COC1=C2C(C(C(C(O)=C(C[C@](C(CO)=O)(O)C[C@@H]3O[C@@]4([H])C[C@H](N)[C@H](O)[C@H](C)O4)C3=C5O)=C5C2=O)=O)=CC=C1.[H]Cl

    Structure Classification
    Initial Source

    Streptomyces peucetius var. Caesius

    Shipping

    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
    Concentration Solvent Mass 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
    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.

    • Molarity Calculator

    • Dilution Calculator

    Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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    Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

    This equation is commonly abbreviated as: C1V1 = C2V2

    Concentration (start)

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    In Vivo:

    Select the appropriate dissolution method based on your experimental animal and administration route.

    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.

    • Protocol 1

      Add each solvent one by one:  5% DMSO    40% PEG300    5% Tween-80    50% Saline

      Solubility: ≥ 2.75 mg/mL (4.74 mM); Clear solution

    • Protocol 2

      Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

      Solubility: ≥ 2.08 mg/mL (3.59 mM); Clear solution

      This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

      Taking 1 mL working solution as an example, add 100 μL DMSO 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.

    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

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    (per animal)

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    Dosing volume
    (per animal)

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    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).
    Purity & Documentation

    Purity: 99.90%

    References

    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 Concentration Solvent Mass 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.

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    • Do most proteins show cross-species activity?

      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.

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    Product Name:
    Doxorubicin hydrochloride
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