Mitoxantrone

SKU: orb1300634

Description

Mitoxantrone is a dual Topo II and PKC inhibitor (IC50=8.5 μM) with established antitumor activity. It is widely used in research models for leukemia, breast cancer, and hepatocellular carcinoma, supporting both in vitro mechanistic studies and in vivo efficacy experiments.

Research Area

Cell Biology, Epigenetics & Chromatin, Infectious Disease & Virology, Metabolism Research, Molecular Biology, Pharmacology & Drug Discovery, Signal Transduction

Key Properties

• CAS Number: 65271-80-9
• MW: 444.48
• Purity: 98.74% (May vary between batches)
• Formula: C₂₂H₂₈N₄O₆
• SMILES: OCCNCCNc1ccc(NCCNCCO)c2C(=O)c3c(O)ccc(O)c3C(=O)c12
• Target: PKC|||Topoisomerase
• Solubility: Ethanol:< 1 mg/mL (insoluble or slightly soluble);5% DMSO+95% Saline:2.37 mg/mL (5.33 mM);H2O:< 1 mg/mL (insoluble or slightly soluble);DMSO:88 mg/mL (197.98 mM);10% DMSO+40% PEG300+5% Tween 80+45% Saline:0.15 mg/mL (0.34 mM)

Bioactivity

• Target IC50:
  MCF-7 cells:1.17 µM|Cancer cells:0.75 nM|C6 cells:10.9 μg/mL|CH1 cells:0.00265 μM|Bel-7402 cells:116.6 nM|HaCaT cells:3.9 μM|A2780 cells:0.00055 μM|PKC:8.5 μM|A375 cells:111.5 nM|Caco-2 cells:1.4 μM|A549 cells:0.036 nM|Daudi cells:0.005 μM|HCT116 cells:0.022 μM|CCRF-CEM cells:0.036 μM|2008 cells:7.8 nM
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• In Vivo:
  Mitoxantrone transiently decreases the growth rate of HID xenografts in mice but does not affect that of PAC120 xenografts. Mitoxantrone results in the severity of the cardiac lesions and the nephropathy and the intestinal toxicity in spontaneously hypertensive rats. Mitoxantrone and iron(III) form a strong 2:1 complex, in which mitoxantrone may be acting as a tridentate ligand.
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• In Vitro:
  Mitoxantrone induces DNA fragmentation and the proteolytic cleavage of poly(ADP-ribose) polymerase (PARP), a marker of the activation of caspases, in all the patients studied, demonstrating that the cytotoxic effect of mitoxantrone is due to induction of apoptosis. Mitoxantrone activates NFkappaB and stimulates IkappaBalpha degradation in the promyelocytic leukemia cell line HL60 but not in the variant cells, HL60/MX2 cells, which lack the beta isoform of topoisomerase II and express a truncated alpha isoform that results in an altered subcellular distribution. Mitoxantrone inhibits proliferation of activated PBMCs, B lymphocytes, or antigen-specific T-cell lines (TCLs) stimulated on antigen-presenting cells (APCs) in a dose-dependent manner. Mitoxantrone induces apoptosis of PBMCs, monocytes and DCs at low concentrations, whereas higher doses causes cell lysis.
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• Cell Research:
  The human breast carcinoma cell lines MDA-MB-231 and MCF-7 are seeded in standard 96-well plates. One day after seeding, the culture medium is changed and replaced by medium containing different concentration of Mitoxantrone (10-5 to 5 μM) with or without DHA (30 μM) during 7 days. Viability of cells are measured as a whole by the tetrazolium salt assay.
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Storage & Handling

• Storage: -20°C
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

Topo II, Topoisomerase, Protein kinase C, PKC, Apoptosis, antitumor, B-CLL cells, breast cancer, NSC-301739, NSC301739, lymphocytes, Mitoxantrone, mitozantrone, Orthopoxvirus, NSC 301739, inhibit, Inhibitor, HL60 cells, MCF-7, leukaemia, Endogenous Metabolite

Compound Identifiers

PubChem CID

4212