Description

Product Description

Busulfan (CAS 55-98-1) is a small-molecule bifunctional alkylating agent belonging to the class of sulfonate esters. Its chemical structure allows the formation of covalent interstrand and intrastrand DNA crosslinks, disrupting replication and transcription in rapidly dividing cells. This mechanism underpins its use as a chemotherapeutic and as a research model to study DNA damage-mediated cytotoxicity.

Physical and Chemical Properties:

• Molecular formula: C8H16O4S4

• Molecular weight: 246.33 g/mol

• Appearance: White crystalline powder

• Solubility: Soluble in DMSO, ethanol, and aqueous buffers

• Stability: Stable at 2–8 °C; sensitive to light and moisture over extended periods

Research Applications:
Busulfan is widely utilized in preclinical studies to model DNA alkylation, apoptosis, and cytotoxicity:

1. DNA Crosslinking Studies: Busulfan forms covalent adducts between guanine bases across complementary DNA strands, creating interstrand crosslinks that interfere with replication fork progression.

2. Apoptosis and Cell Cycle Research: By triggering DNA damage response (DDR), Busulfan activates p53-dependent pathways, upregulates cyclin-dependent kinase inhibitors, and induces caspase-mediated programmed cell death.

3. Drug Resistance Mechanisms: It is used to study nucleotide excision repair (NER), base excision repair (BER), and mismatch repair (MMR) in chemotherapeutic resistance models.

4. Combination Therapy Modeling: Busulfan serves as a standard agent for evaluating synergistic effects of combination regimens with other chemotherapeutic or targeted molecules.

5. In Vivo Models: Preclinical studies in murine and hematopoietic models use Busulfan to investigate marrow ablation, stem cell transplantation, and systemic cytotoxicity.

6. Cellular and Molecular Pathways: Research often focuses on DDR signaling, reactive oxygen species (ROS) induction, mitochondrial perturbation, and modulation of apoptotic proteins such as Bcl-2 family members.

Experimental Considerations:

• Handling: Powder should be managed with gloves, lab coat, and eye protection.

• Dosing: Concentrations are chosen based on cell type and experimental goals; cytotoxic effects are dose-dependent.

• Solvent Compatibility: Compatible with DMSO, ethanol, and aqueous buffers; solubility should be verified in intended experimental conditions.

Busulfan’s reproducible mechanism, high purity (≥99%), and well-characterized cytotoxic profile make it an indispensable tool for research in DNA damage, chemotherapeutic modeling, apoptosis induction, and drug resistance studies.

Product Specifications

Mechanism of Action

Busulfan exerts its effects as a bifunctional alkylating agent, covalently binding to N7 positions of guanine residues on DNA, forming interstrand and intrastrand crosslinks. These crosslinks:

1. Prevent DNA replication and transcription, stalling replication forks.

2. Activate DNA damage response (DDR) pathways, including ATM/ATR kinases.

3. Induce p53-dependent cell cycle arrest at G1/S and G2/M checkpoints.

4. Trigger apoptosis via caspase activation, mitochondrial perturbation, and ROS generation.

Research Insights:

• Interstrand crosslinks are highly cytotoxic; they require specialized repair pathways, allowing study of nucleotide excision repair (NER) and homologous recombination.

• DNA adduct formation by Busulfan is dose- and time-dependent, offering a reproducible model for studying chemotherapeutic kinetics.

• Busulfan is frequently used in combination with other DNA-damaging agents to investigate synergy, resistance, and repair pathway modulation.

• In hematopoietic stem cell research, Busulfan-induced myeloablation is a standard model for evaluating engraftment and bone marrow transplantation outcomes.

Comparative Studies:

• Compared to other alkylating agents (e.g., cyclophosphamide, melphalan), Busulfan exhibits unique bifunctional crosslinking properties and lower systemic toxicity in experimental models.

• Studies comparing Busulfan to platinum compounds highlight differences in DNA adduct structure, repair sensitivity, and apoptotic signaling activation.

  

Side Effects

For laboratory research, Busulfan should be handled with care:

• Toxicity: Cytotoxic effects include apoptosis, cell cycle arrest, DNA fragmentation, and mitochondrial dysfunction. Effects are dose-dependent and vary by cell type.

• Handling Safety: Use gloves, lab coat, protective eyewear, and work in a fume hood. Avoid inhalation, ingestion, and skin/eye contact.

• Environmental Precautions: Dispose of any waste according to institutional chemical safety protocols.

• Long-term Stability: Powder is stable at 2–8 °C but may degrade if exposed to light, moisture, or high temperatures for extended periods.

• Experimental Observations:

  • In vitro: DNA crosslinking, cytotoxicity in cancer cell lines, apoptosis induction.

  • In vivo: Myeloablation, stem cell depletion, dose-dependent cytotoxicity.

Busulfan is strictly for research use only and should not be administered to humans or animals outside regulated experimental settings.

Keywords

 CAS 55-98-1, alkylating agent, DNA crosslinking, apoptosis induction, cell cycle arrest, chemotherapeutic cytotoxicity, preclinical cancer research, DNA damage response, high purity, ≥99% purity, factory peptide supplier, peptide wholesale China, China peptide manufacturer, OEM & bulk peptide production.

Shipping Guarantee

All shipments of Busulfan are handled with validated cold-chain logistics to ensure compound stability and integrity. The powder is sealed in moisture-proof, light-protected containers with secondary protective wrapping. Packages are shipped with full tracking, insurance coverage, and international courier support.

Trade Assurance

Busulfan authenticity is guaranteed, analytically verified using HPLC, MS, and NMR. Each batch comes with a Certificate of Analysis (CoA) confirming ≥99% purity. Trade assurance covers replacement or refund in case of deviation from listed specifications. Quality, batch consistency, and shipping conditions are strictly monitored.

Payment Support

We provide secure, global payment options including PayPal, major credit cards (Visa, MasterCard, American Express), telegraphic transfer (T/T), and cryptocurrencies (USDT, Bitcoin, Ethereum). All transactions are encrypted and verified to ensure confidentiality and fund protection.

Disclaimer

This product is intended for laboratory research use only. It is not for human or veterinary administration. Users must follow standard safety protocols. Data generated with Busulfan should not be interpreted as clinical guidance or therapeutic advice.

References

1. PubChem Database: Busulfan (CID 24495)↗

2. ChEMBL Database: Busulfan Bioactivity Summary (ChEMBL ID CHEMBL193)↗

3. DrugBank: Busulfan – DB00390↗

4. PubMed ID 17960907 – Busulfan mechanism of DNA crosslinking and cytotoxicity↗

5. IUPHAR/BPS Guide to Pharmacology: Busulfan target profile↗