Doxorubicin (Adriamycin)

Licensed by Pfizer Catalog No.S1208 Synonyms: NSC 123127

Doxorubicin (Adriamycin) Chemical Structure

Molecular Weight(MW): 579.98

Doxorubicin (Adriamycin) is an antibiotic agent that inhibits DNA topoisomerase II and induces DNA damage and apoptosis in tumor cells.

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Cited by 28 Publications

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  • Enhancement of apoptotic response by addition of targeted agents lapatinib and sunitinib to doxorubicin in the same device reservoir at 24 hours. P values were determined using Student’s t test for all graphs.

    Sci Transl Med, 2015, 7(284): 284ra57 . Doxorubicin (Adriamycin) purchased from Selleck.

    Cell viabilities with increasing concentrations of cisplatin (CP) and doxorubicin (DOXO) under normoxic and hypoxic condition for 48 hours were determined by MTT assay. IC50 values are presented as the means ?SDs (n=4) and * denotes p<0.05.

    Cancer Res 2014 74, 298-308. Doxorubicin (Adriamycin) purchased from Selleck.

  •  

    Doxorubicin release of P(MAA-g-EG) and P(MAA-g-EG) containing nanoparticles in two-step pH conditions. Doxorubicinloaded P(MAA-g-EG) ,P(MAA-g-EG)-1.0NP ,P(MAA-g-EG)-2.5NP, and P(MAA-g-EG)-5.0NP crushed particles (75–150 um) were released in 1 PBS (pH 2.0) for 90 min. Then the pH was increased to 7.0 by adding 5N NaOH and release continued for 6 h.

    J Biomed Mater Res Part A 2012 10.1002/jbm.a.34064. Doxorubicin (Adriamycin) purchased from Selleck.

    Temporal uptake of free DOX or DOX-PCL63-b-PNVP90 micelles into K-562 (I) and DL (J) cells were studied by incubating in 24-well plates at a concentration of 50,000 cells per well. Representative images shown were obtained using a fluorescence microscope Eclipse 80i (Nikon, Japan) (Plan Fluor, 40X, NA 0.75 objective) equipped with blue and red filters for, Hoechst and Doxorubicin respectively (n = 3).

    PLoS One 2014 9, e94309. Doxorubicin (Adriamycin) purchased from Selleck.

  • PLoS One 2013 8(1), e54595. Doxorubicin (Adriamycin) purchased from Selleck.

    CON+ -positive control (with FBS as chemoattractant); CON- - negative control (without chemoattractant); DOX -doxorubicin; WZ -WZ811; PF- PF-573228; * -significant difference compared to positive control: p<0.05; ** -significant difference compared to positive control: p<0.01; # -significant difference between combination and inhibitor only: p<0.05. Cancer cell invasion was analyzed using Transwell membranes assembled in 24-well plates and covered with a layer of Matrigel. COR-L23 cells were treated for 24 h with 50 nM DOX, 10 uM WZ811, 5 uM PF-573228 and combinations of inhibitors with 50 nM DOX. Similarly, RH460 cells were treated for 24 h with 1 uM DOX, 10 uM WZ811, 2.5 uM PF-573228 and combinations of inhibitors with 1 uM DOX. Applied doses were the ones that exerted the most pronounced synergistic effect on cytotoxicity level. After the incubation period, cells that invaded through matrigel and membranes were fixed in 4% paraformaldehyde-PBS and stained with Hoechst 33342 nuclear stain. Cells were visualized and counted under a fluorescent microscope at 10x magnification.

    2014 Dr Milica Pesic from Institute for Biological Research. Doxorubicin (Adriamycin) purchased from Selleck.

Purity & Quality Control

Choose Selective Topoisomerase Inhibitors

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Notes:

2. For more details, such as half maximal inhibitory concentrations (IC50s) and working concentrations of each inhibitor, please click on the link of the inhibitor of interest.
3. "+" indicates inhibitory effect. Increased inhibition is marked by a higher "+" designation.
4. Orange "√" refers to compounds which do inhibitory effects on the related isoform, but without specific value.

Biological Activity

Description Doxorubicin (Adriamycin) is an antibiotic agent that inhibits DNA topoisomerase II and induces DNA damage and apoptosis in tumor cells.
Targets
Topo II [1]
(Tumor cells)
In vitro

Doxorubicin, an antibiotic anthracycline, is commonly considered to exert its anti-tumor activity at two fundamental levels, altering DNA and producing free radicals to trigger apoptosis of cancer cells through DNA damage. Doxorubicin can block the synthesis of DNA by intercalating into the DNA strand, and inhibits DNA topoisomerase II (TOP2). Doxorubicin is most effective when cells are rapidly proliferating and expressing high levels of TOP2. Additionally, Doxorubicin can trigger apoptosis by producing ceramide (which prompts apoptosis by activating p53 or other downstream pathways such as JNK), the degradation of Akt by serine threonine proteases, the mitochondrial release of cytochrome c, increased FasL (death receptor Fas/CD95 ligand) mRNA production, and a greater production of free radicals. [2] Pre-treatment with GSNO (nitrosoglutathione) suppresses the resistance in the doxorubicin-resistant breast cancer cell line MCF7/Dx, accompanied by enhanced protein glutathionylation and accumulation of doxorubicin in the nucleus. [3] Doxorubicin induced G2/M checkpoint arrest are attributed to elevated cyclin G2 (CycG2) expression and phospho-modification of proteins in the ataxia telangiectasia mutated (ATM) and ATM and Rad3-related (ATR) signaling pathways. [5] Doxorubicin inhibits AMP-activated protein kinase (AMPK), resulting in SIRT1 dysfunction, p53 accumulation, and increased cell death in mouse embryonic fibroblasts (MEFs) and cardiomyocytes, which can be further sensitized by pre-inhibition of AMPK. [6] Doxorubicin elicits a marked heat shock response, and that either inhibition or silencing of heat shock proteins enhance the Doxorubicin apoptotic effect in neuroblastoma cells. Nanomolar Doxorubicin treatment of neuroblastoma cells causes dose-dependent over-ubiquitination of a specific set of proteins in the absence of measurable inhibition of proteasome, and loss of activity of ubiquitinated enzymes such as lactate dehydrogenase and α-enolase, the protein ubiquination patterns of which is similar to those with proteasome inhibitor Bortezomib, indicating that Doxorubicin may also exert its effect by damaging proteins. [8]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
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LNcaP NGH0VlBHfW6ldHnvckBCe3OjeR?= NFfFboo{KM7:TR?= MViyOEBp MX3JcoNz\WG|ZTDv[kBkdGWjdnXkJINie3Cjc3WtPUBt\X[nbB?= MkPDNlQxQTVyOEm=
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LB647-SCLC MUTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4LMO2lEPTB;MUKzMlM2KG6P MlPtV2FPT0WU
NCI-H1703 NIXMS4lIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYfJR|UxRTF{Nj60NkBvVQ>? NGnyR3BUSU6JRWK=
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RPMI-7951 MWDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MlLKTWM2OD1zM{CuNVQhdk1? MWLTRW5ITVJ?
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NCI-H64 MnTQS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYHJR|UxRTF|Mj62OUBvVQ>? M{jGd3NCVkeHUh?=
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NCI-H747 NHT3RYFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYXMPYtxUUN3ME2xN|UvODJibl2= M{fyfnNCVkeHUh?=
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JiyoyeP-2003 NVvMb|ZZT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVfWZVRZUUN3ME2xN|cvQCCwTR?= MVHTRW5ITVJ?
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NCI-H748 M33ob2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVvJR|UxRTF2Nz6zNUBvVQ>? M3XvTXNCVkeHUh?=
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BB65-RCC NWWzfZQ6T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGi1elFKSzVyPUG0PU4{OSCwTR?= NYi5O2JqW0GQR1XS
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JVM-3 MX7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4e4VGlEPTB;ND62NFYyQCEQvF2= MlvFV2FPT0WU
ECC4 NXfvdnFLT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFHpTWJKSzVyPUSuO|Y2PDFizszN MVTTRW5ITVJ?
MDA-MB-453 MlS1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MUnJR|UxRTRwOEWxN|Qh|ryP MU\TRW5ITVJ?
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DMS-53 NYrjWVlxT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVu4fGVUUUN3ME22MlE4OTB4IN88US=> Mo[5V2FPT0WU
LB771-HNC NIr1Zm1Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NI\HNpRKSzVyPU[uOFY5ODZizszN M3LyOnNCVkeHUh?=
BB49-HNC NXK3WG5OT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXrJR|UxRTdwNEG3PVEh|ryP NFywcZVUSU6JRWK=
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SW684 M13PNmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVXJR|UxRTN2LkG1OlEh|ryP NIrxW|NUSU6JRWK=
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NCI-H720 M2XZTmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4LpR2lEPTB;NEGuPVczPiEQvF2= M1Sz[HNCVkeHUh?=
P31-FUJ MmjMS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MlHSTWM2OD12ND6zNlg1KM7:TR?= MWrTRW5ITVJ?
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... Click to View More Cell Line Experimental Data

In vivo In vivo, Doxorubicin in combination with adenoviral MnSOD (AdMnSOD) plus 1,3-bis(2-chloroethyl)-1-nitrosourea (BCNU) has the greatest effect in decreasing the volumes of MB231 tumors and prolonging survival of mice. [1] Although its use is limited by the chronic and acute toxic side effects it produces, Doxorubicin is essential in treating breast and oesophageal carcinomas, solid tumours in childhood, osteosarcomas, Kaposi's sarcoma, soft tissue sarcomas, and Hodgkin and non-Hodgkin lymphomas. [2]

Protocol

Animal Research
+ Expand
  • Animal Models: Female athymic nude mice injected s.c. with MB231 cells
  • Formulation: Dissolved in DMSO, and diluted in saline
  • Dosages: 3 mg/kg/day
  • Administration: Delivered intratumorly
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 100 mg/mL (172.41 mM) warming
Water 20 mg/mL (34.48 mM)
Ethanol <1 mg/mL
In vivo

* 1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 579.98
Formula

C27H29NO11.HCl

CAS No. 25316-40-9
Storage powder
in solvent
Synonyms NSC 123127

Bio Calculators

Molarity Calculator

Molarity Calculator

Calculate the mass, volume or concentration required for a solution. The Selleck molarity calculator is based on the following equation:

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

  • Mass
    Concentration
    Volume
    Molecular Weight

*When preparing stock solutions, please always use the batch-specific molecular weight of the product found on the via label and MSDS / COA (available on product pages).

Dilution Calculator

Dilution Calculator

Calculate the dilution required to prepare a stock solution. The Selleck dilution calculator is based on the following equation:

Concentration (start) x Volume (start) = Concentration (final) x Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2 ( Input Output )

  • C1
    V1
    C2
    V2

* When preparing stock solutions always use the batch-specific molecular weight of the product found on the vial label and MSDS / COA (available online).

The Serial Dilution Calculator Equation

  • Serial Dilutions

  • Computed Result

  • C1=C0/X C1: LOG(C1):
    C2=C1/X C2: LOG(C2):
    C3=C2/X C3: LOG(C3):
    C4=C3/X C4: LOG(C4):
    C5=C4/X C5: LOG(C5):
    C6=C5/X C6: LOG(C6):
    C7=C6/X C7: LOG(C7):
    C8=C7/X C8: LOG(C8):
Molecular Weight Calculator

Molecular Weight Calculator

Enter the chemical formula of a compound to calculate its molar mass and elemental composition:

Total Molecular Weight: g/mol

Tip: Chemical formula is case sensitive. C10H16N2O2 c10h16n2o2

Instructions to calculate molar mass (molecular weight) of a chemical compound:

To calculate molar mass of a chemical compound, please enter its chemical formula and click 'Calculate'.

Definitions of molecular mass, molecular weight, molar mass and molar weight:

Molecular mass (molecular weight) is the mass of one molecule of a substance and is expressed in the unified atomic mass units (u). (1 u is equal to 1/12 the mass of one atom of carbon-12)
Molar mass (molar weight) is the mass of one mole of a substance and is expressed in g/mol.

Molarity Calculator

Mass Concentration Volume Molecular Weight

Clinical Trial Information

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT02839707 Not yet recruiting Fallopian Tube Clear Cell Adenocarcinoma|Fallopian Tube Endometrioid Adenocarcinoma|High Grade Fallopian Tube Serous Adenocarcinoma|High Grade Ovarian Serous Adenocarcinoma|Ovarian Clear Cell Adenocarcinoma|Ovarian Endometrioid Adenocarcinoma|Ovarian Seromucinous Carcinoma|Primary Peritoneal High Grade Serous Adenocarcinoma|Recurrent Fallopian Tube Carcinoma|Recurrent Ovarian Carcinoma|Recurrent Primary Peritoneal Carcinoma|Undifferentiated Fallopian Tube Carcinoma|Undifferentiated Ovarian Carcinoma National Cancer Institute (NCI) May 2017 Phase 2|Phase 3
NCT02743065 Not yet recruiting Hepatocellular Carcinoma Fifth Affiliated Hospital, Sun Yat-Sen University|Third Affiliated Hospital, Sun Yat-Sen University September 2016 --
NCT01775475 Not yet recruiting AIDS-related Diffuse Large Cell Lymphoma|AIDS-related Diffuse Mixed Cell Lymphoma|AIDS-related Diffuse Small Cleaved Cell Lymphoma|AIDS-related Immunoblastic Large Cell Lymphoma|AIDS-related Lymphoblastic Lymphoma|AIDS-related Peripheral/Systemic Lymphoma|AIDS-related Small Noncleaved Cell Lymphoma|Stage III AIDS-related Lymphoma|Stage IV AIDS-related Lymphoma AIDS Malignancy Consortium|National Cancer Institute (NCI)|The EMMES Corporation September 2016 Phase 2
NCT02783599 Not yet recruiting Soft Tissue Sarcoma Eli Lilly and Company September 2016 Phase 1
NCT02685657 Not yet recruiting Triple Negative Breast Cancer Russian Academy of Medical Sciences|Russian Society of Clinical Oncology September 2016 Phase 2
NCT02723994 Not yet recruiting B-cell Acute Lymphoblastic Leukemia Incyte Corporation|Childrens Oncology Group August 2016 Phase 2

Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

Tel: +1-832-582-8158 Ext:3

If you have any other enquiries, please leave a message.

  • * Indicates a Required Field

Frequently Asked Questions

  • Question 1:

    Why the IC50 of the compound varied over time in our measurement?

  • Answer:

    Sometimes the IC50 value might vary between different batch of compounds due to the slight differences in purity. If different IC50 was seen in the same batch of compound, the problem may lies in the process of dissolvement. Make sure that you see no particles and the solution is clear with your stock solution.

Topoisomerase Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID