Doxorubicin (Adriamycin) HCl

For research use only.

Licensed by Pfizer Catalog No.S1208 Synonyms: NSC 123127, DOX, Doxorubicin hydrochloride, Hydroxydaunorubicin HCl

738 publications

Doxorubicin (Adriamycin) HCl Chemical Structure

CAS No. 25316-40-9

Doxorubicin (Adriamycin, NSC 123127, DOX, Hydroxydaunorubicin) HCl is an antibiotic agent that inhibits DNA topoisomerase II and induces DNA damage, mitophagy and apoptosis in tumor cells. Doxorubicin reduces basal phosphorylation of AMPK. Doxorubicin is used in the concomitant treatment of HIV-infected patients but is found to be at high risk of HBV reactivation.

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Selleck's Doxorubicin (Adriamycin) HCl has been cited by 738 publications

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Biological Activity

Description Doxorubicin (Adriamycin, NSC 123127, DOX, Hydroxydaunorubicin) HCl is an antibiotic agent that inhibits DNA topoisomerase II and induces DNA damage, mitophagy and apoptosis in tumor cells. Doxorubicin reduces basal phosphorylation of AMPK. Doxorubicin is used in the concomitant treatment of HIV-infected patients but is found to be at high risk of HBV reactivation.
Targets
AMPK [6]
()
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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K052 M1S0Wmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVjJR|UxRTJzLkS0NVgh|ryP MVu8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQly1N|Q3Oy9pPmPBUmdGWjxxYU6=
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RCC10RGB M3Pa[Wdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MoDHTWM2OD1|MD6wOlEyKM7:TR?= MV:8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQly1N|Q3Oy9pPmPBUmdGWjxxYU6=
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SNU-C1 NXTVdYpDT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWPJR|UxRTN{LkSxO|Uh|ryP NI\3d3c9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmw2OzR4Mz:nQnNCVkeHUkyvZV4>
C32 MoHGS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYrCS4xUUUN3ME2zNk45PzJizszN M1j0[FxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFU{PDZ|Lze+V2FPT0WUPD;hQi=>
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NCI-H720 NF\nc2FIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NIXTWmJKSzVyPUSxMlk4OjZizszN MVu8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQly1N|Q3Oy9pPmPBUmdGWjxxYU6=
P31-FUJ NWDXeZJOT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWXIZYVTUUN3ME20OE4{Ojh2IN88US=> M1HxZVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFU{PDZ|Lze+V2FPT0WUPD;hQi=>
NCI-H524 NH6zV5RIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGn2b3VKSzVyPUS4MlgzPDhizszN MmLJQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMOVM1PjNxJ{7TRW5ITVJ:L3G+

... Click to View More Cell Line Experimental Data

Assay
Methods Test Index PMID
Western blot
POU5F1 / SOX2 / NANOG; 

PubMed: 27929731     


NT2/D1 cells treated with 10 nM of doxorubicin were subjected to WB analysis for pluripotency factors (POU5F1, NANOG, SOX2) and differentiation markers (TUBB3).

ATG5 / ATG7 / SQSTM1 / LC3A-II / LC3B-II / p-mTOR; 

PubMed: 27929731     


NT2/D1 cells treated with 10 nM of doxorubicin were subjected to WB analysis for autophagy markers (ATG5, ATG7, SQSTM1, LC3A-II, LC3B-II and p-MTOR). 

P62 / LC3II; 

PubMed: 28208617     


(A,B) Doxorubicin induces autophagy in pancreatic cancer cells. Western blot analysis of LC3-II and p62 protein levels in Mia PaCa-2 and Panc-1 cell lines treated with indicated concentrations of doxorubicin for 24 h, or treated with 2.5 μM doxorubicin for indicated times.

p-AKT(T308) / p-Akt(S473) / Akt / p-PRAS40(T246) / PRAS40 / p-H2A.X(S139); 

PubMed: 26027929     


MCF10A cells were serum-starved and treated with (A) 2 μM doxorubicin over a 10 hour time course.

27929731 28208617 26027929
Growth inhibition assay
Cell viability; 

PubMed: 25871400     


Salinomycin enhances the cytotoxicity of doxorubicin in HCC cellsRelative cell viability (mean ± SD) for salinomycin (black), doxorubicin (blue) and doxorubicin plus salinomycin (red) in HuH-7, HepG2, SNU-449 and SNU-387 cells.

25871400
Immunofluorescence
LC3; 

PubMed: 24970805     


Doxorubicin induces GFP-LC3 puncta formation in hepatocellular carcinoma cells. SK-Hep1 cells were treated with doxorubicin (2.5 μM) or CQ (10 μM) plus doxorubicin for 7 h and cells were examined with a confocal microscope for GFP-LC3 punctuation/aggregation.

24970805
ELISA
OPN; 

PubMed: 24963635     


A549 were exposed to 50 nM doxorubicin or PBS for 48 h. OPN concentrations in cell culture media were determined by ELISA.

24963635
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:[1]
- Collapse
  • Animal Models: Female athymic nude mice injected s.c. with MB231 cells
  • Dosages: 3 mg/kg/day
  • Administration: Delivered intratumorly
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 100 mg/mL warmed (172.41 mM)
Water 20 mg/mL (34.48 mM)
Ethanol 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, DOX, Doxorubicin hydrochloride, Hydroxydaunorubicin HCl
Smiles CC1C(C(CC(O1)OC2CC(CC3=C2C(=C4C(=C3O)C(=O)C5=C(C4=O)C(=CC=C5)OC)O)(C(=O)CO)O)N)O.Cl

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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 interventions Conditions Sponsor/Collaborators Start Date Phases
NCT04874311 Not yet recruiting Drug: Bintrafusp alfa|Drug: Doxorubicin Advanced Soft-tissue Sarcoma|Metastatic Soft-tissue Sarcoma Institut Bergonié|Merck Healthcare KGaA Darmstadt Germany an affiliate of Merck KGaA Darmstadt Germany December 2021 Phase 2
NCT04852367 Not yet recruiting Device: Focused Ultrasound|Drug: Doxorubicin|Drug: ThermoDox Pancreatic Ductal Adenocarcinoma|Pancreatic Cancer Stage IV|Pancreatic Cancer Non-resectable|Pancreatic Cancer Metastatic University of Oxford|Oncology Clinical Trials Office|National Institute for Health Research United Kingdom|Celsion May 2021 Phase 1
NCT04204941 Recruiting Drug: Tazemetostat|Drug: Placebo|Drug: Doxorubicin HCl Advanced Soft Tissue Sarcoma|Advanced Epithelioid Sarcoma Epizyme Inc. December 19 2019 Phase 3
NCT03975205 Not yet recruiting Drug: Doxorubicin Lymphoma Leukemia Sutphin Drugs|Bharath Charitable Cancer Hospital and Institute July 1 2019 Early Phase 1
NCT03719430 Recruiting Drug: Doxorubicin|Drug: APX005M Soft Tissue Sarcoma Columbia University|Apexigen Inc. March 20 2019 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

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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.

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID