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Doxorubicin

MCE China：Doxorubicin

Brand：MedChemExpress (MCE)

Cat. No.HY-15142A

CAS：23214-92-8

Synonyms：Hydroxydaunorubicin

Storage：Please store the product under the recommended conditions in the Certificate of Analysis.

Shipping：Room temperature in continental US; may vary elsewhere.

Description：Doxorubicin (Hydroxydaunorubicin), a broad-spectrum anthracycline antibiotic with cytotoxic properties, is an anti-cancer chemotherapy agent. Doxorubicin has fluorescence properties. Doxorubicin inhibits topoisomerase II with an IC50 of 2.67 μM, thus stopping DNA replication. Doxorubicin reduces basal phosphorylation of AMPK and its downstream target acetyl-CoA carboxylase. Doxorubicin induces apoptosis and autophagy. Doxorubicin inhibits human DNA topoisomerase I with an IC50 of 0.8 μM.

In Vitro：Combination of Doxorubicin (Hydroxydaunorubicin) and Simvastatin (HY-17502) in the highest tested concentrations (2 μM and 10 μM, respec-tively) kills 97% of the Hela cells[4]. Doxorubicin can label neuron cells, and it is bright red under Rhodamine filter bag, and light red-orange under catecholamine filter bag[8]. Doxorubicin (5 μM; 10-30 min) can be accumulated in B16-F10 melanoma cell line CRL-6475 in a time-dependent manner, and can be detected by green or red fluorescence (green fluorescence has higher detection sensitivity) with a maximum excitation wavelength (λex) and a maximum emission wavelength (λem) of 470 nm and 560 nm, respectively[10].

In Vivo：Doxorubicin (4-8 mg/kg) can delay tumor growth and reduce the expression of c-FLIP in PC3 xenograft nude mice. Doxorubicin (Intraperitoneal injection; single dose (10 mg/kg) / once daily for 10 days (1 mg/kg) / once per week for 5 weeks (2 mg/kg)) has cardiotoxicity in Sprague-Dawley rats, but compared with a single dose of 10 mg/kg, cumulative dosing of 10 mg/kg over several days or weeks can increase the survival rate of rats.[6] Doxorubicin (4%-20%; Intrastriatal injection; Single dose) is neurotoxic in Sprague-Dawley rats[8]. Doxorubicin can be coupled to gold nanoparticles (Au NPs) by PH-sensitive bonding under acidic conditions, allowing it to pass through the blood-brain barrier with a maximum absorption wavelength of 528 nm[9].

IC50 & Target：Topoisomerase I 0.8 μM (IC50) Topoisomerase II 2.67 μM (IC50) Daunorubicins/Doxorubicins HIV-1

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References：

[1]. Nitiss JL, et al. Targeting DNA topoisomerase II in cancer chemotherapy.Nat Rev Cancer. 2009 May;9(5):338-50.  [Content Brief]

[2]. Rhee HK, et al. Synthesis, cytotoxicity, and DNA topoisomerase II inhibitory activity of benzofuroquinolinediones. Bioorg Med Chem. 2007 Feb 15;15(4):1651-8.  [Content Brief]

[3]. Foglesong PD, et al. Doxorubicin inhibits human DNA topoisomerase I. Cancer Chemother Pharmacol. 1992;30(2):123-5.  [Content Brief]

[4]. Sadeghi-Aliabadi H, et al. Cytotoxic evaluation of doxorubicin in combination with simvastatin against human cancer cells. Res Pharm Sci. 2010 Jul;5(2):127-33.  [Content Brief]

[5]. El-Zawahry A, et al. Doxorubicin increases the effectiveness of Apo2L/TRAIL for tumor growth inhibition of prostate cancerxenografts. BMC Cancer. 2005 Jan 7;5:2.  [Content Brief]

[6]. Hayward R, et al. Doxorubicin cardiotoxicity in the rat: an in vivo characterization. J Am Assoc Lab Anim Sci. 2007 Jul;46(4):20-32.  [Content Brief]

[7]. Johansson S, et al. Elimination of HIV-1 infection by treatment with a doxorubicin-conjugated anti-envelope antibody. AIDS. 2006;20(15):1911-1915.  [Content Brief]

[8]. Koda LY, Van der Kooy D. Doxorubicin: a fluorescent neurotoxin retrogradely transported in the central nervous system. Neurosci Lett. 1983 Mar 28;36(1):1-8. doi: 10.1016/0304-3940(83)90476-7. PMID: 6190113. 9  [Content Brief]

[9]. Mirza A Z, Shamshad H. Preparation and characterization of doxorubicin functionalized gold nanoparticles[J]. European journal of medicinal chemistry, 2011, 46(5): 1857-1860.

[10]. Kauffman MK, Kauffman ME, Zhu H, Jia Z, Li YR. Fluorescence-Based Assays for Measuring Doxorubicin in Biological Systems. React Oxyg Species (Apex). 2016;2(6):432-439. doi: 10.20455/ros.2016.873. PMID: 29707647; PMCID: PMC5921830.  [Content Brief]