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Mitoxantrone

Catalog No. T6588   CAS 65271-80-9
Synonyms: mitozantrone

Mitoxantrone (mitozantrone) is an anthracenedione antibiotic with antineoplastic activity. Mitoxantrone intercalates into and crosslinks DNA, thereby disrupting DNA and RNA replication. This agent also binds to topoisomerase II, resulting in DNA strand breaks and inhibition of DNA repair. Mitoxantrone is less cardiotoxic compared to doxorubicin.

All products from TargetMol are for Research Use Only. Not for Human or Veterinary or Therapeutic Use.
Mitoxantrone Chemical Structure
Mitoxantrone, CAS 65271-80-9
Pack Size Availability Price/USD Quantity
25 mg In stock $ 33.00
50 mg In stock $ 47.00
100 mg In stock $ 65.00
200 mg In stock $ 109.00
1 mL * 10 mM (in DMSO) In stock $ 50.00
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Purity: 98.14%
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Biological Description
Chemical Properties
Storage & Solubility Information
Description Mitoxantrone (mitozantrone) is an anthracenedione antibiotic with antineoplastic activity. Mitoxantrone intercalates into and crosslinks DNA, thereby disrupting DNA and RNA replication. This agent also binds to topoisomerase II, resulting in DNA strand breaks and inhibition of DNA repair. Mitoxantrone is less cardiotoxic compared to doxorubicin.
Targets&IC50 PKC:8.5 μM.
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. [1] 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. [2] 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. [3]
In vivo Mitoxantrone transiently decreases the growth rate of HID xenografts in mice but does not affect that of PAC120 xenografts. [4] 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. [5]
Kinase Assay activity-based protein profiling (ABPP): Mouse brains are Dounce-homogenized in PBS, pH7.5, followed by a low-speed spin (1,400×, 5 min) to remove debris. The supernatant is then subjected to centrifugation (64,000×, 45 min) to provide the cytosolic fraction in the supernatant and the membrane fraction as a pellet. The pellet is washed and resuspended in PBS buffer by sonication. Total protein concentration in each fraction is determined using a protein assay kit. Samples are stored at -80 °C until use. Mouse brain membrane proteomes, are diluted to 1 mg/mL in PBS and pre-incubated with varying concentrations of inhibitors (1 nM to 10 mM) for 30 min at 37 °C before the addition of FP-rhodamine at a final concentration of 2 mM in a 50 mL total reaction volume. After 30 min at 25 °C, the reactions are quenched with 4×SDS-PAGE loading buffer, boiled for 5 min at 90 °C, subjected to SDS-PAGE and visualized in-gel using a flatbed fluorescence s
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[3].
Synonyms mitozantrone
Molecular Weight 444.48
Formula C22H28N4O6
CAS No. 65271-80-9

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

Ethanol: < 1 mg/mL (insoluble or slightly soluble)

DMSO: 88 mg/mL (197.98 mM)

H2O: < 1 mg/mL (insoluble or slightly soluble)

TargetMolReferences and Literature

1. Bellosillo B, et al. Br J Haematol, 1998, 100(1), 142-146. 2. Boland MP, et al. J Biol Chem, 2000, 275(33), 25231-25238. 3. Neuhaus O, et al. J Neuroimmunol, 2005, 168(1-2), 128-137. 4. Oudard S, et al. J Urol, 2003, 169(5), 1729-1734. 5. Herman EH, et al. J Mol Cell Cardiol, 1997, 29(9), 2415-2430. 6. Dong L, Shen S, Chen W, et al. Discovery of Novel Inhibitors Targeting Human O-GlcNAcase: Docking-Based Virtual Screening, Biological Evaluation, Structural Modification, and Molecular Dynamics Simulation[J]. Journal of chemical information and modeling. 2019, 59(10): 4374-4382. 7. Zeng X, Zhu S, Lu W, et al. Target identification among known drugs by deep learning from heterogeneous networks[J]. Chemical Science. 2020, 11(7): 1775-1797.

TargetMolCitations

1. Zeng X, Zhu S, Lu W, et al. Target identification among known drugs by deep learning from heterogeneous networks. Chemical Science. 2020, 11(7): 1775-1797. 2. Dong L, Shen S, Chen W, et al. Discovery of Novel Inhibitors Targeting Human O-GlcNAcase: Docking-Based Virtual Screening, Biological Evaluation, Structural Modification, and Molecular Dynamics Simulation. Journal of chemical information and modeling. 2019, 59(10): 4374-4382. 3. Zeng R, Yang X M, Li H W, et al.Simplified Derivatives of Tetrandrine as Potent and Specific P-gp Inhibitors to Reverse Multidrug Resistance in Cancer Chemotherapy.Journal of Medicinal Chemistry.2023 4. Ba D, Li H, Liu R, et al.Exploratory study on the efficacy of bortezomib combining mitoxantrone or CD22-CAR T therapy targeting CD19-negative relapse after CD19-CAR T cell therapy with a simpler cell-line-based model.Apoptosis.2023: 1-12.

Related compound libraries

This product is contained In the following compound libraries:
Anti-Cancer Drug Library Anti-Cancer Active Compound Library TGF-beta/Smad Compound Library Anti-Cancer Approved Drug Library Anti-Cancer Clinical Compound Library Anti-Breast Cancer Compound Library Inhibitor Library Reprogramming Compound Library Clinical Compound Library Pediatric Drug Library

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Keywords

Mitoxantrone 65271-80-9 Chromatin/Epigenetic Cytoskeletal Signaling DNA Damage/DNA Repair Topoisomerase PKC leukaemia NSC301739 MCF-7 NSC 301739 lymphocytes HL60 cells NSC-301739 B-CLL cells Protein kinase C inhibit Orthopoxvirus antitumor Endogenous Metabolite Apoptosis breast cancer Inhibitor mitozantrone inhibitor

 

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