Mitoxantrone is an anthraquinone that intercalates in DNA and inhibits topoisomerase II (IC50 = 5.3 μM), thus inhibiting cell proliferation. It also inhibits HIV-1 integrase (IC50 = 3.8 μM). Mitoxantrone is exported from cells in an ATP- and glutathione-dependent manner by multidrug resistance protein-1.4 Formulations containing mitoxantrone have been used in the treatment of cancer and multiple sclerosis.
CAS Number: 70476-82-3
Molecular Weight: 517.40
Chemical Name: 1,4-dihydroxy-5,8-bis((2-((2-hydroxyethyl)amino)ethyl)amino)anthracene-9,10-dione dihydrochloride
Appearance: Solid Power.
Purity: ≥98% (or refer to the Certificate of Analysis)
Solubility: Soluble in DMSO, not in water
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis
Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.
Shelf Life: ≥12 months if stored properly.
Stock Solution Storage: 0 - 4 oC for 1 month or refer to the Certificate of Analysis.
Drug Formulation: To be determined.
HS Tariff Code: 382200
How to use
Mitoxantrone inhibits PKC in a competitive manner with respect to histone H1, and its Ki value is 6.3 μM and in a non-competitive manner with respect to phosphatidylserine and ATP. Treatment of B-CLL cells for 48 h with mitoxantrone (0.5 μg/mL) induces a decrease in cell viability. Mitoxantrone induces DNA fragmentation and the proteolytic cleavage of poly(ADP-ribose) polymerase (PARP), demonstrating that the cytotoxic effect of mitoxantrone is due to induction of apoptosis. Mitoxantrone shows cytotoxicity to human breast carcinoma cell lines MDA-MB-231 and MCF-7 with IC50 values of 18 and 196 nM, respectively.
Mitoxantrone given IP at the optimal dose (1.6 mg/kg/day; as a free base) produces a statistically significant number of 60-day survivors (curative effect) in mice with IP implanted L1210 leukemia. In SC implanted Lewis lung carcinoma, mitoxantrone and ADM administered IV also shows effective antitumor activities and produces a 60% and a 45% ILS, respectively.
- Kapoor T, Mehan S. Neuroprotective methodologies in treatment of Multiple Sclerosis: Current status of Clinical and Pre-clinical findings. Curr Drug Discov Technol. 2020 Feb 6. doi: 10.2174/1570163817666200207100903. [Epub ahead of print] PubMed PMID: 32031075.
- Djeni TN, Kouame KH, Ake FDM, Amoikon LST, Dje MK, Jeyaram K. Microbial Diversity and Metabolite Profiles of Palm Wine Produced From Three Different Palm Tree Species in Côte d'Ivoire. Sci Rep. 2020 Feb 3;10(1):1715. doi: 10.1038/s41598-020-58587-2. PubMed PMID: 32015447.
- Lin KN, Jiang YL, Zhang SG, Huang SY, Li H. Grape seed proanthocyanidin extract reverses multidrug resistance in HL-60/ADR cells via inhibition of the PI3K/Akt signaling pathway. Biomed Pharmacother. 2020 Jan 30;125:109885. doi: 10.1016/j.biopha.2020.109885. [Epub ahead of print] PubMed PMID: 32007917.
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