Doxorubicin HCL

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

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  Cancer Res. 2024 May 8.

  HDAC Inhibition Increases CXCL12 Secretion to Recruit Natural Killer Cells in Peripheral T Cell Lymphoma | Cancer Research | American Association for Cancer Research
  Doxorubicin HCL purchased from AbMole

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  ACS Appl Mater Interfaces. 2024 Feb;16(6):6868-6878.

  Doxorubicin-Loaded Microalgal Delivery System for Combined Chemotherapy and Enhanced Photodynamic Therapy of Osteosarcoma
  Doxorubicin HCL purchased from AbMole

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  Phytomedicine. 2024 Jan;126:155395.

  Bufalin suppresses hepatocellular carcinogenesis by targeting M2 macrophage-governed Wnt1/β-catenin signaling
  Doxorubicin HCL purchased from AbMole

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  ACS Appl Bio Mater. 2024 Sep 06.

  Doxorubicin-Loaded Ultrasmall Gold Nanoparticles (1.5 nm) for Brain Tumor Therapy and Assessment of Their Biodistribution
  Doxorubicin HCL purchased from AbMole

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  Eng. Regen. 2024 Mar.

  Microalgae-based drug delivery system for tumor microenvironment photo-modulating and synergistic chemo-photodynamic therapy of osteosarcoma
  Doxorubicin HCL purchased from AbMole

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  Elife. 2021 Jun 28;10:e65150.

  Resistance to different anthracycline chemotherapeutics elicits distinct and actionable primary metabolic dependencies in breast cancer
  Doxorubicin HCL purchased from AbMole

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  Mol Med Rep. 2021 Mar;23(3):219.

  Shengxian decoction decreases doxorubicin‑induced cardiac apoptosis by regulating the TREM1/NF‑κB signaling pathway
  Doxorubicin HCL purchased from AbMole

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  2020 Aug.

  Blockage of AMPK-ULK1 pathway mediated autophagy promotes cell apoptosis to increase doxorubicin sensitivity in breast cancer (BC) cells: an in vitro study
  Doxorubicin HCL purchased from AbMole

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  PLoS One. 2017 Jul 13;12(7):e0181340.

  Development and characterization of a human three-dimensional chondrosarcoma culture for in vitro drug testing
  Doxorubicin HCL purchased from AbMole

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  Biomaterials. 2012 Jun;4345-52.

  Antitumor efficacy following the intracellular and interstitial release of liposomal doxorubicin
  Doxorubicin HCL purchased from AbMole

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

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.