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Doxorubicin HCL

Cat. No. M1969
Doxorubicin HCL Structure
Synonym:

RP 13057 hydrochloride; Adriamycin; Rubex;DOX

Size Price Availability Quantity
Free Sample (0.5-1 mg)  USD 0 In stock
20mg USD 30  USD30 In stock
50mg USD 50  USD50 In stock
100mg USD 70  USD70 In stock
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Quality Control & Documentation
Biological Activity

Doxorubicin (Adriamycin) HCl is an antineoplastic agent used in the treatment of a wide range of cancers, including hematological malignancies, many types of carcinoma, and soft tissue sarcomas. Doxorubicin interacts with DNA by intercalation and inhibition of macromolecular biosynthesis. Doxorubicin stabilizes the topoisomerase II complex after it has broken the DNA chain for replication, preventing the DNA double helix from being resealed and thereby stopping the process of replication. In studies with isolated nuclei, adriamycin was also a more potent inhibitor of DNA synthesis than RNA synthesis. However, with intact cells, adriamycin inhibited both DNA and RNA synthesis to about the same extent. The inhibition produced by adriamycin on RNA synthesis in intact cells was greater than that observed in the cell-free systems. Adriamycin inhibited protein synthesis in a cell-free system consisting of polyribosomes, transfer RNA, and enzymes but did not inhibit protein synthesis in intact cells. Combination therapy experiments with sirolimus (rapamycin) and doxorubicin have shown promise in treating Akt-positive lymphomas in mice.

Product Citations
Customer Product Validations & Biological Datas
Source Ther Deliv (2015). Figure 2. Doxorubicin HCl
Method equilibrium dialysis
Cell Lines HeLa cells
Concentrations 1 mg/ml
Incubation Time 24 h
Results Similar to the effect of acyl chain length on the release rate of doxorubicin, PEGylation of the liposome tended to decrease the release rate.
Source Ther Deliv (2015). Figure 1. Doxorubicin HCl
Method WST-8 assay
Cell Lines HeLa cells
Concentrations 1.0 μg/ml
Incubation Time 24 h
Results Cytotoxicity and intracellular uptake of doxorubicin were not positively correlated in liposomes no. 2–5, 13–15 and 16–18.
Protocol (for reference only)
Cell Experiment
Cell lines Human choriocarcinoma cell line
Preparation method Briefly, cells were plated on 96-well plates (10,000 cells/well) and a day after (cell culture 80% confluent) were exposed to doxorubicin (0–8 mM), L-DOX (0–8 mM) or PL-DOX (0–200 mM) in non-supplemented serum-free growth medium for 4 h. After exposure, the cells were washed and further incubated for 20 h.
Concentrations 0–8 µM
Incubation time 24 h
Animal Experiment
Animal models Male Sprague-Dawley rats
Formulation
Dosages 4 mg/kg
Administration i.v.
Chemical Information
Molecular Weight 579.98
Formula C27H29NO11.HCl
CAS Number 25316-40-9
Solubility (25°C) DMSO 45 mg/mL
Water 30 mg/mL
Storage 2-8°C, protect from light, dry, sealed
Conversion of different model animals based on BSA (PMID: 27057123)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.

References

[1] Zhang J, et al. Br J Pharmacol. Cellular pharmacokinetic mechanisms of adriamycin resistance and its modulation by 20(S)-ginsenoside Rh2 in MCF-7/Adr cells.

[2] David J Burkhart, et al. J Med Chem. Design, synthesis, and preliminary evaluation of doxazolidine carbamates as prodrugs activated by carboxylesterases

[3] Suvara K Wattanapitayakul, et al. Basic Clin Pharmacol Toxicol. Screening of antioxidants from medicinal plants for cardioprotective effect against doxorubicin toxicity

[4] Momparler RL, et al. Cancer Res. Effect of adriamycin on DNA, RNA, and protein synthesis in cell-free systems and intact cells.

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Keywords: Doxorubicin HCL, RP 13057 hydrochloride; Adriamycin; Rubex;DOX supplier, Animal Modeling, inhibitors, activators


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