(Synonyms: Hydroxydaunorubicin, DOX, Adriamycin) Copy Product Info
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Synonyms: Hydroxydaunorubicin, DOX, Adriamycin
Catalog No. T1456 Copy Product Info
Purity: 99.88%
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Doxorubicin (Adriamycin) is a fluorescent anthracycline antitumor antibiotic that inhibits Topoisomerase I/II, induces apoptosis and autophagy, downregulates the AMPK signaling pathway, and is commonly used in cancer chemotherapy as well as in models of nephritis and heart failure.
Cas No. 23214-92-8
Other Forms of Doxorubicin:
Doxorubicin hydrochloride (Standard)
Doxorubicin-13C,D3 Trifluoroacetate Salt (Standard)
Doxorubicin hydrochloride
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Purity:99.88%
Appearance:Solid
Color:Red
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Product Information
Bioactivity
Description
Doxorubicin (Adriamycin) is a fluorescent anthracycline antitumor antibiotic that inhibits Topoisomerase I/II, induces apoptosis and autophagy, downregulates the AMPK signaling pathway, and is commonly used in cancer chemotherapy as well as in models of nephritis and heart failure.
Targets & IC50
Topo II:2.67 μM (IC50), Topo I:0.8 μM (IC50)
In vitro
The combination of Doxorubicin and Simvastatin at the highest tested concentrations (2 μM and 10 μM, respec-tively) kills 97% of the Hela cells[2].
In vivo
In an experiment, mice with PC3 xenografts received injections of Doxorubicin at dosages of 2, 4, or 8 mg/kg, and tumor volume was monitored. The 2 mg/kg dose did not inhibit tumor growth, but doses of 4 mg/kg and 8 mg/kg initially delayed growth, significantly reducing c-FLIP levels in the tumors (p<0.05 on days 18 and 22)[3]. In a separate study with rats, treatments involved a single intraperitoneal injection of 10 mg/kg Doxorubicin, ten daily injections of 1 mg/kg, or five weekly injections of 2 mg/kg, resulting in an 80% mortality rate by day 28 for the first group, and on days 107 and 98 for the latter groups, respectively. Furthermore, fractional shortening—a measure of heart function—decreased by 30% in the first group at week 2, 55% in the second group at week 13, and 42% in the third group at week 13[4].
Synonyms
Hydroxydaunorubicin, DOX, Adriamycin
Disease Modeling Protocol
Cardiomyopathy model
Modeling Mechanism：
Doxorubicin (DOX) induces cardiac damage through multiple pathways: ① It triggers oxidative stress, inhibiting NRF2-mediated antioxidant pathways (downregulation of genes such as NRF2, GST, and HO-1), leading to the accumulation of reactive oxygen species (ROS) and lipid peroxidation; ② It interferes with the protein ubiquitination system, disrupting cardiomyocyte protein homeostasis; ③ It inhibits the PI3K/AKT signaling pathway, promoting cardiomyocyte apoptosis and necrosis; ④ It damages mitochondrial function, affecting energy metabolism, ultimately leading to myocardial hypertrophy, fibrosis, and decreased cardiac function.
Related Products：
Doxorubicin (T1456)
Modeling Method：
Experimental Subject：
Rats, Sprague-Dawley, Female
Dosage and Administration Route：
15 mg/kg Doxorubicin, dissolved in physiological saline, intraperitoneal injection (i.p.)
Dosing Frequency and Duration Model：
Single dose
Validation：
1. Pathological Indicators: - Myocardial Injury: HE staining showed myocardial cell degeneration and necrosis; Masson staining revealed interstitial fibrosis. - Hematological Changes: Lymphopenia and thrombocytopenia were observed (48 hours after modeling). 2. Molecular Indicators: - Gene Expression: 2411 genes were synchronously differentially expressed (SDRG) in myocardial and peripheral blood mononuclear cells (PBMCs), including downregulation of antioxidant genes such as NRF2 (-2.085-fold) and HO-1 (-2.849-fold), and upregulation of S100A8/A9 (calcium-binding protein). - Signaling Pathways: Western blot showed decreased expression of PI3K/AKT pathway-related proteins and disordered expression of ubiquitination-related molecules. 3. Biochemical Indicators: - Serum Markers: Decreased albumin (ALB), increased alanine aminotransferase (ALT), total bilirubin (TBIL), and creatinine (CRE) (48 hours after modeling). - Tissue Drug Concentration: DOX in myocardial tissue. The concentration reached 0.342±0.22 μg/mg protein (p=0.051), and the blood concentration reached 0.591±0.041 μg/ml (p<0.01); 4. Functional indicators: - Cardiac function: Echocardiography of the chronic model showed a decrease in left ventricular ejection fraction (LVEF) and abnormal diastolic function.
*Precautions： All rats were euthanized within 48 hours of DOX administration under deep isoflurane anesthesia.
*References：Todorova VK,et,al. Transcriptome profiling of peripheral blood cells identifies potential biomarkers for doxorubicin cardiotoxicity in a rat model. PLoS One. 2012;7(11):e48398.
Cell Research
Doxorubicin is dissolved in stock solutions (1 mM) and serially diluted with RPMI 1640 media (0.1, 1, and 2 μM)[2]. 160 μL of Hela cells suspension (3×104 cell/mL) is dispensed into three 96-well U-bottom microplates and incubated for 24 h at
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