Doxorubicin (Adriamycin) 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. Adriamycin-induced congestive heart failure (CHF) can best be prevented by limiting the total dose as follows: 400 to 450 mg per sq meter following mediastinal radiation and 500 to 550 mg per sq meter for patients without other significant risk factors. Combination therapy experiments with sirolimus (rapamycin) and doxorubicin have shown promise in treating Akt-positive lymphomas in mice.
|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.|
|Incubation time||24 h|
|Animal models||Male Sprague-Dawley rats|
|Body Surface Area (m2)||0.007||0.025||0.15||0.05||0.02||0.5|
|Animal A (mg/kg) = Animal B (mg/kg) multiplied by||Animal B Km|
|Animal A Km|
For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 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 resveratrol of 11.2 mg/kg.
|Solubility||DMSO 100 mg/mL|
Biomaterials 2012 Jun;4345-52.
Antitumor efficacy following the intracellular and interstitial release of liposomal doxorubicin
Doxorubicin HCL purchased from AbMole
Cellular pharmacokinetic mechanisms of adriamycin resistance and its modulation by 20(S)-ginsenoside Rh2 in MCF-7/Adr cells.
Zhang J, et al. Br J Pharmacol. 2012 Jan;165(1):120-34. PMID: 21615726.
Effect of adriamycin on DNA, RNA, and protein synthesis in cell-free systems and intact cells.
Momparler RL, et al. Cancer Res. 1976 Aug;36(8):2891-5. PMID: 1277199.
|Related Topoisomerase Products|
Pirarubicin Hcl is an analogue of the anthracycline anti-neoplastic doxorubicin, which is an inhibitor of Topo II.
Ofloxacin is a synthetic broad-spectrum antimicrobial agent.
Novobiocin Sodium is an aminocoumarin antibiotic that targets bacterial DNA gyrase (TopoIV), used to treat susceptible gram positive bacteria.
Norfloxacin is a broad-spectrum antibiotic.
Nitroxoline is a urinary antibacterial agent active against susceptible gram-positive and gram-negative organisms commonly found in urinary tract infections. It is a fluorquinolone that is active against bacterial gyrases.
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