Description

Product Description

Nimustine Hydrochloride Injection is a synthetic nitrosourea derivative classified as a potent alkylating agent. It plays a vital role in experimental oncology and neuro-oncology due to its unique capability to cross the blood-brain barrier and selectively accumulate in neural tissues. Researchers utilize Nimustine to investigate cellular and molecular pathways associated with DNA damage, repair inhibition, and programmed cell death (apoptosis).

Chemically, Nimustine Hydrochloride (1-(4-amino-2-methyl-5-pyrimidinyl)methyl-3-(2-chloroethyl)-3-nitrosourea hydrochloride) belongs to the same pharmacological class as carmustine (BCNU) and lomustine (CCNU), yet demonstrates distinct pharmacokinetic and biological properties. The compound is soluble in water, ethanol, and methanol, and appears as a white to slightly yellow crystalline powder. It is highly reactive under light and moisture, hence requiring storage in dark and dry conditions at low temperatures.

In research applications, Nimustine Hydrochloride Injection serves as a benchmark for studying chemotherapeutic drug behavior in central nervous system malignancies, particularly glioblastoma multiforme (GBM). It provides a foundation for understanding DNA alkylation, double-strand break formation, and downstream activation of apoptotic cascades. Its dual chemical reactivity — alkylating and carbamoylating — contributes to its broad spectrum of cytotoxic effects in tumor research.

Research Significance

Nimustine Hydrochloride Injection’s importance in preclinical research lies in its ability to simulate the pharmacodynamics of clinical alkylating therapies. Its high lipophilicity allows researchers to study CNS penetration and neurotoxicity, while its defined molecular mechanism offers reproducibility across experiments. It is used as a model compound in comparative studies evaluating next-generation anticancer molecules, DNA repair enzyme inhibitors, and synergistic radiochemotherapy regimens.

Furthermore, Nimustine’s role extends to genetic and epigenetic studies focused on MGMT (O6-methylguanine-DNA methyltransferase) regulation — a critical factor determining nitrosourea resistance in tumor cells. Understanding this interaction provides key insights into personalized oncology research and targeted therapy development.

Product Specifications

Mechanism of Action

Nimustine Hydrochloride functions as a bifunctional alkylating agent, producing cytotoxicity through two principal mechanisms: DNA alkylation and protein carbamoylation. Upon administration, it undergoes spontaneous decomposition to generate chloroethyl carbocations and isocyanates. The chloroethyl groups attack nucleophilic sites within DNA, forming covalent crosslinks primarily at the N7 position of guanine bases. These crosslinks disrupt the helical integrity of DNA, inhibit replication and transcription, and ultimately trigger apoptosis.

The carbamoylating action of Nimustine further contributes to its cytotoxicity by modifying lysine residues in proteins, including DNA repair enzymes. This dual mechanism ensures sustained DNA damage, thereby amplifying the apoptotic response. Research indicates that Nimustine’s alkylation triggers DNA double-strand breaks, activating p53, caspase-3, and other pro-apoptotic signaling pathways.

Crossing the Blood-Brain Barrier

One of Nimustine Hydrochloride’s defining attributes is its high lipophilicity, allowing it to penetrate the blood-brain barrier (BBB). This property enables research on brain tumors, particularly gliomas and medulloblastomas. In comparative models, Nimustine exhibits superior CNS distribution compared to carmustine, making it ideal for preclinical studies involving brain-targeted chemotherapeutic delivery.

Combination Research

In cancer pharmacology, Nimustine is frequently investigated in combination with radiotherapy, cisplatin, or temozolomide to evaluate synergistic cytotoxic effects. Such studies have demonstrated enhanced DNA damage, greater oxidative stress, and increased apoptosis in tumor cell lines. The compound’s ability to augment radiation-induced DNA strand breaks provides a valuable tool for understanding multimodal therapy in oncology research.

Molecular Pathways and Resistance

Nimustine also plays a key role in elucidating resistance pathways. Overexpression of MGMT, mismatch repair (MMR) deficiencies, and mutations in p53 are among the primary mechanisms leading to alkylator resistance. By studying Nimustine’s interactions within these systems, researchers can design next-generation inhibitors to overcome chemoresistance.

Side Effects

Nimustine Hydrochloride Injection, as observed in preclinical models, demonstrates a range of toxicological effects consistent with alkylating agents. These observations are critical for understanding its safety profile and optimizing dosing strategies in laboratory research.

• Myelosuppression: A dose-dependent decrease in hematopoietic cell proliferation leading to leukopenia and thrombocytopenia.

• Hepatotoxicity: Elevated hepatic enzyme levels observed in long-term exposure models.

• Nephrotoxicity: Nitrosourea metabolites can cause renal tubular dysfunction and proteinuria.

• Neurotoxicity: Its ability to cross the BBB makes it a model for CNS toxicity studies; research notes demyelination and neuronal apoptosis under certain conditions.

• Pulmonary Fibrosis: Chronic exposure may induce lung tissue damage.

• Gastrointestinal Stress: Laboratory animals show nausea, vomiting, and diarrhea under acute exposure scenarios.

Although these effects are dose-dependent and context-specific, they serve as crucial indicators of Nimustine’s bioactivity and help researchers refine analog design and drug safety models.

Keywords

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Shipping Guarantee

All shipments are handled using validated cold-chain logistics to preserve compound integrity. Each package is sealed in moisture-proof containers with secondary protective wrapping and continuous temperature monitoring. Products are shipped via express international couriers with full tracking and insurance coverage.

Trade Assurance

We ensure product authenticity, verified ≥99% purity, and compliance with analytical standards (HPLC, MS, and NMR). Each batch is supplied with a Certificate of Analysis (CoA). Our trade assurance policy guarantees replacement or refund for any deviation from listed specifications.

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Disclaimer

All products are intended for laboratory research use only. Not for human use, diagnostic, or therapeutic applications. Handle with appropriate protective equipment and in accordance with institutional safety regulations.