Description

Product Description

1. Molecular Characteristics and Formulation

Mitoxantrone Hydrochloride Injection (CAS 70476-82-3) is a synthetic anthracenedione compound with potent antineoplastic activity. It functions as a DNA intercalator and topoisomerase II inhibitor, inducing double-strand DNA breaks, cell cycle arrest, and apoptosis. The injectable formulation is prepared under GMP-compliant conditions, ensuring high purity, chemical stability, and reproducible pharmacological effects. Supplied as a sterile aqueous solution, it supports precise dosing in both in vitro cytotoxicity studies and in vivo preclinical models.

2. Antineoplastic Mechanism

Mitoxantrone Hydrochloride binds DNA intercalatively, stabilizing topoisomerase II-DNA cleavable complexes and preventing DNA religation. This results in accumulation of DNA strand breaks, triggering p53-dependent apoptosis, cell cycle arrest in G2/M phase, and inhibition of cell proliferation. It is widely applied to study leukemia, lymphoma, breast cancer, and prostate cancer preclinical models.

3. Immunomodulatory Applications

Beyond its cytotoxic effects, Mitoxantrone Hydrochloride exhibits immunomodulatory activity, making it suitable for research in autoimmune diseases such as multiple sclerosis (MS). It selectively depletes pathogenic T cells and B cells, modulates cytokine expression, and preserves regulatory immune populations, providing a mechanistic tool for studying immune-mediated pathologies.

4. Metabolic and Cellular Research Applications

Mitoxantrone is used to investigate DNA damage response pathways, apoptosis mechanisms, and cell cycle regulation. It enables studies on drug resistance mechanisms, topoisomerase II dynamics, and genotoxic stress responses in diverse cancer cell lines and primary cultures. Researchers can combine it with flow cytometry, Western blotting, and transcriptomic assays to assess cellular responses to DNA damage and cytotoxic stress.

5. Pharmacological Research and Preclinical Models

Mitoxantrone Hydrochloride Injection serves as a reference standard in pharmacology, pharmacokinetics (PK), and pharmacodynamics (PD) research. It supports dose-response studies, toxicity assays, and combination therapy evaluations. Integration with animal models allows simulation of drug metabolism, tissue distribution, and therapeutic efficacy in both hematologic and solid tumor preclinical studies.

Product Specifications

Mechanism of Action

1. DNA Intercalation

Mitoxantrone Hydrochloride functions primarily as a DNA intercalator, inserting between base pairs of double-stranded DNA. This intercalation disrupts DNA helical structure, impeding DNA replication and transcription. The resulting structural perturbations trigger DNA damage response pathways, making it a reliable tool for studying genotoxic stress and apoptotic mechanisms in preclinical research.

2. Topoisomerase II Inhibition

Mitoxantrone selectively inhibits topoisomerase II, a key enzyme that mediates DNA strand break religation during replication. By stabilizing the topoisomerase II-DNA cleavable complex, it prevents repair of DNA double-strand breaks, leading to accumulation of DNA damage. This mechanism underlies its cytotoxic effect on rapidly dividing cells and is widely applied in cancer biology research, including leukemia, lymphoma, and solid tumor models.

3. Induction of Apoptosis and Cell Cycle Arrest

DNA damage induced by Mitoxantrone activates p53-dependent and independent pathways, resulting in G2/M cell cycle arrest and programmed cell death. Researchers use it to study apoptotic signaling cascades, including caspase activation, Bcl-2 family modulation, and mitochondrial depolarization, providing mechanistic insights into chemotherapeutic cytotoxicity.

4. Immunomodulatory Effects

In addition to direct cytotoxicity, Mitoxantrone Hydrochloride Injection exhibits immunomodulatory properties. It selectively affects T cells, B cells, and other immune subsets, reducing pathogenic immune populations while sparing regulatory cells. This property is exploited in autoimmune disease models such as multiple sclerosis, enabling investigation of immune-mediated pathology, cytokine regulation, and therapeutic mechanisms.

5. Applications in DNA Damage and Drug Resistance Studies

Mitoxantrone is a critical tool for studying DNA damage response (DDR) pathways, topoisomerase II dynamics, and drug resistance mechanisms. By inducing controlled genotoxic stress, researchers can explore cellular repair mechanisms, checkpoint activation, and apoptosis thresholds. It is also used in combination therapy experiments to evaluate synergistic cytotoxic effects and potential resistance mechanisms in preclinical oncology research.

6. Experimental Pharmacology and Translational Research

The well-characterized mechanism of action makes Mitoxantrone Injection suitable for pharmacokinetic (PK) and pharmacodynamic (PD) studies, including dose-response assays, tissue distribution, and bioavailability assessments. It provides a reference standard for experimental antineoplastic agents, enabling reproducible validation of assay protocols and preclinical therapeutic strategies.

Applications

1. Preclinical Oncology Research

Mitoxantrone Hydrochloride Injection is widely used in preclinical cancer research to investigate antineoplastic mechanisms, cytotoxicity, and tumor cell apoptosis. Its ability to intercalate DNA and inhibit topoisomerase II makes it a reliable tool for studying cell cycle arrest, DNA damage response, and tumor cell proliferation in leukemia, lymphoma, breast cancer, and prostate cancer models. Researchers utilize it to evaluate dose-dependent cytotoxic effects, combinatorial therapies, and mechanisms of drug resistance.

2. Hematologic Malignancy Models

In hematologic research, Mitoxantrone is employed to study leukemia and lymphoma pathophysiology. It induces double-strand DNA breaks, leading to apoptosis in rapidly dividing hematopoietic cells. Experimental models often combine flow cytometry, cytogenetic analysis, and molecular assays to quantify cell cycle arrest, apoptosis markers, and DNA damage responses.

3. Immunomodulation and Autoimmune Disease Studies

Mitoxantrone Hydrochloride exhibits selective immunomodulatory effects, making it useful in autoimmune disease research such as multiple sclerosis (MS) and systemic lupus erythematosus (SLE). It depletes pathogenic T and B cells, modulates cytokine secretion, and preserves regulatory immune populations, enabling mechanistic studies of immune-mediated tissue damage.

4. Cell Cycle and Apoptosis Research

Researchers utilize Mitoxantrone to investigate cell cycle dynamics, apoptosis pathways, and DNA repair mechanisms. Its action induces G2/M arrest and caspase-dependent apoptosis, allowing detailed studies on checkpoint regulation, Bcl-2 family modulation, and mitochondrial pathways. This is essential for drug screening, combination therapy evaluations, and understanding chemoresistance mechanisms.

5. Pharmacological and Translational Studies

As a well-characterized antineoplastic agent, Mitoxantrone Injection serves as a reference for pharmacokinetics (PK), pharmacodynamics (PD), and dose-response studies. It supports evaluation of novel topoisomerase II inhibitors, biosimilars, and experimental anticancer compounds in both in vitro and in vivo models. Researchers can assess tissue distribution, metabolic stability, and therapeutic indices for translational research.

6. Drug Resistance and Mechanistic Investigations

Mitoxantrone is employed to study drug resistance mechanisms, particularly topoisomerase II-mediated resistance and multidrug resistance (MDR) pathways. Researchers can combine it with efflux pump inhibitors, checkpoint modulators, or DNA repair pathway inhibitors to elucidate resistance mechanisms and optimize preclinical therapeutic strategies.

7. Biomolecular and Genotoxicity Studies

Its precise action on DNA and topoisomerase II allows researchers to study DNA damage response (DDR), genomic instability, and genotoxicity assays. Mitoxantrone is commonly used with comet assays, γ-H2AX staining, and transcriptomic profiling to assess cellular responses to DNA damage and mechanistic pathways of apoptosis.

Side Effects

1. In Vitro Experimental Observations

In cell culture studies, Mitoxantrone Hydrochloride Injection is generally well-tolerated at recommended concentrations. Excessive doses may cause off-target cytotoxicity, including non-specific DNA damage and altered cell viability in non-target cell lines. Researchers should optimize concentration and exposure time to ensure specific topoisomerase II inhibition while minimizing unintended cellular effects.

2. In Vivo Animal Models

In preclinical animal studies, Mitoxantrone may induce:

• Myelosuppression: reduction in white blood cells, red blood cells, and platelets

• Cardiotoxicity risk: particularly with high cumulative doses or prolonged administration

• Gastrointestinal effects: mild anorexia, weight loss, or diarrhea in sensitive models

• Bone marrow suppression: requiring careful monitoring of hematologic parameters

These effects are dose-dependent and typically reversible in short-term studies. Researchers should design experiments to monitor hematologic indices and cardiac function markers.

3. Immunomodulatory and Inflammatory Effects

Mitoxantrone Hydrochloride can transiently modulate T cell, B cell, and macrophage populations in animal models. While useful for autoimmune disease studies, excessive dosing may alter cytokine profiles or cause unintended immune suppression, potentially confounding experimental results.

4. Metabolic and Systemic Effects

In vivo administration may influence hepatic enzyme activity and metabolic pathways, including mild alterations in liver function markers or glucose metabolism in certain models. Researchers should account for these systemic effects when interpreting metabolic or toxicity studies.

5. Experimental Precautionary Measures

To minimize side effects and experimental artifacts:

• Use recommended dosing and exposure durations

• Monitor hematologic parameters, liver enzymes, and cardiac markers in long-term animal studies

• Handle Mitoxantrone Injection under Biosafety Level 2 (BSL-2) conditions

• Avoid excessive repeated dosing in sensitive models

• Store at 2–8°C, protect from light, and prevent repeated freeze-thaw cycles to maintain biological activity

Mitoxantrone Hydrochloride Injection is intended for research use only and should not be used for human or veterinary clinical applications outside controlled experimental models.

Keywords

Mitoxantrone Hydrochloride Injection, CAS 70476-82-3, anthracenedione antineoplastic agent, DNA intercalator, topoisomerase II inhibitor, cytotoxic agent, apoptosis inducer, cell cycle arrest, hematologic malignancy research, leukemia model, lymphoma model, breast cancer preclinical studies, prostate cancer research, immune modulation, autoimmune disease model, genotoxicity studies, pharmacology research, preclinical oncology, experimental antineoplastic drug, injectable solution

Shipping Guarantee

• Cold-Chain Shipping: All Mitoxantrone Hydrochloride Injection orders are shipped under 2–8°C temperature-controlled conditions to preserve chemical stability and biological activity.

• Packaging: Sterile vials are secured with thermal insulation and protective casing to prevent damage and light exposure.

• Tracking: Each shipment includes tracking information for real-time monitoring.

• Delivery Assurance: Guaranteed intact, sterile, and pharmacologically active product upon arrival.

Trade Assurance

• Factory-Direct Supply: Sourced from GMP-compliant manufacturers with stringent quality control.

• Lot-to-Lot Consistency: All batches validated with COA, TDS, MSDS to ensure reproducibility.

• Global Compliance: Meets international standards for research-grade antineoplastic agents.

• Customer Protection: Buyers are covered under trade agreements ensuring on-time delivery and product integrity.

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• Multiple Payment Options: T/T, PayPal, Western Union, and major international credit cards accepted.

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• Flexible Terms: Support for bulk orders, custom concentrations, and prepayment arrangements.

Disclaimer

Mitoxantrone Hydrochloride Injection (CAS 70476-82-3) is intended for research use only. It is not approved for human or veterinary clinical use. Researchers must adhere to institutional safety protocols, local regulations, and proper laboratory handling procedures. The manufacturer and supplier disclaim liability for misuse or clinical application outside controlled experimental conditions.

References

1. Gluck S. Mitoxantrone in the treatment of leukemia and lymphoma: mechanism and applications. Leuk Res. 1997;21:499–508. Link

2. Hartung HP, et al. Mitoxantrone in multiple sclerosis: mechanism of immunomodulation. Ann Neurol. 2002;51:71–78. Link

3. Weiss RB. Anthracenedione antineoplastic agents: pharmacology and toxicology. Cancer Treat Rev. 1992;19:77–96. Link

4. Curt GA, et al. Mechanistic studies of Mitoxantrone: DNA intercalation and topoisomerase II inhibition. Biochem Pharmacol. 1988;37:453–460. Link

5. Kantarjian HM, et al. Preclinical evaluation of Mitoxantrone in leukemia models. Blood. 1987;70:1105–1112. Link