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CAS No.: 1342820-68-1
Cat No.: BADC-00738
4.5 
MA-PEG4-VA-PBD is a drug-linker conjugate for ADC by using PBD (Pyrrolobenzodiazepine dimers, a potent antitumor antibiotic), linked via MA-PEG4-VA.
Structure of 1342820-68-1
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MA-PEG4-VA-PBD is a versatile compound primarily used in the development of targeted cancer therapies, particularly antibody-drug conjugates (ADCs). The maleimide (MA) group allows for efficient conjugation to biomolecules containing thiol groups, such as antibodies or peptides. The PEG4 (polyethylene glycol) spacer enhances the solubility and stability of the conjugate, improving its pharmacokinetics. The VA (valine-alanine) linker is designed to be cleaved in the intracellular environment, ensuring that the cytotoxic payload, PBD (Pyrrolo[2,1-c][1,4]benzodiazepine), is released inside the target cell. PBD is a potent DNA crosslinker that interferes with DNA replication and transcription, leading to apoptosis. This combination of components makes MA-PEG4-VA-PBD a promising candidate for targeted drug delivery in oncology.
One of the main applications of MA-PEG4-VA-PBD is in the development of ADCs for targeted cancer therapy. By attaching the potent cytotoxic agent PBD to an antibody via the maleimide-PEG4-VA linker system, the drug is selectively delivered to cancer cells that express specific surface antigens. The linker is designed to be cleaved once the ADC enters the target cell, allowing for the release of PBD inside the cell. Upon release, PBD crosslinks DNA, disrupting the normal function of the DNA helix and leading to cell cycle arrest and programmed cell death. This targeted delivery system significantly improves the therapeutic index of the drug by minimizing systemic toxicity and maximizing the cytotoxic effect on tumor cells.
MA-PEG4-VA-PBD also plays a critical role in drug resistance studies and the optimization of ADC design. Researchers can utilize this conjugate to investigate how tumor cells develop resistance to chemotherapeutic agents and identify strategies to overcome this resistance. By modifying the linker, payload, or antibody targeting moiety, new ADC formulations can be tested for improved efficacy. This could lead to the development of ADCs with enhanced potency or the ability to bypass mechanisms of drug resistance, providing more effective treatments for resistant cancer strains.
Beyond oncology, MA-PEG4-VA-PBD may have potential applications in the treatment of other diseases where targeted therapy is beneficial. The flexibility of the maleimide-PEG4-VA linker system allows for the attachment of various targeting molecules, making it adaptable for the treatment of infectious diseases, autoimmune disorders, or inflammatory conditions. By coupling MA-PEG4-VA-PBD to peptides or antibodies that recognize specific disease markers, this conjugate could provide a new approach to the targeted delivery of cytotoxic agents in non-cancerous applications, expanding its therapeutic potential.
| Catalog | Product Name | CAS | Inquiry |
|---|---|---|---|
| BADC-00340 | PBD dimer | 1222490-34-7 | |
| BADC-00015 | MC-Val-Ala-PBD | 1342820-51-2 | |
| BADC-01669 | VA-PAB-PBD | 1595275-60-7 | |
| BADC-00670 | Mal-PEG4-VA-PBD | 2259318-50-6 | |
| BADC-00826 | Aniline-MPB-amino-C3-PBD | 2412923-79-4 | |
| BADC-00827 | Py-MPB-amino-C3-PBD | 2412924-07-1 | |
| BADC-01377 | Pyrrolobenzodiazepine (PBD) | 945490-09-5 | |
| BADC-00755 | DBCO-PEG4-VA-PBD |
What is MA-PEG4-VA-PBD?
MA-PEG4-VA-PBD is a cleavable linker-payload conjugate used in antibody-drug conjugates (ADCs). It consists of a valine-alanine dipeptide linker attached to a PBD payload, facilitating targeted cytotoxic delivery upon enzymatic cleavage in tumor cells.
7/2/2023
Dear team, how does MA-PEG4-VA-PBD function in ADCs?
MA-PEG4-VA-PBD functions by connecting a cytotoxic PBD molecule to an antibody through a valine-alanine linker. Upon internalization into target cells, the linker is enzymatically cleaved, releasing the active payload to exert cytotoxicity specifically in malignant cells.
28/11/2020
Dear team, what stability considerations should we be aware of for MA-PEG4-VA-PBD?
MA-PEG4-VA-PBD exhibits high plasma stability due to the PEG4 spacer and peptide linker structure. The conjugate is designed to resist premature cleavage in circulation while ensuring efficient payload release within target cells via lysosomal proteases.
9/10/2021
May I ask which types of antibodies are compatible with MA-PEG4-VA-PBD?
MA-PEG4-VA-PBD is compatible with a wide range of monoclonal antibodies, including IgG1 and IgG2 isotypes. The chemical design allows conjugation via lysine or cysteine residues, enabling flexible ADC development strategies.
12/8/2021
Dear team, what applications is MA-PEG4-VA-PBD commonly used for?
MA-PEG4-VA-PBD is primarily applied in preclinical and clinical ADC research targeting hematologic and solid tumors. Its high potency and selective cleavage profile support the development of therapeutics requiring precise delivery of highly cytotoxic payloads.
19/9/2020
— Dr. Emily Thompson, Senior Research Scientist (USA)
We needed a reliable linker for our ADC development, and MA-PEG4-VA-PBD exceeded expectations in purity and consistency. Delivery was timely and well-packaged.
9/10/2021
— Prof. Lucas Meyer, Biochemist (Germany)
The batch we received of MA-PEG4-VA-PBD was remarkably uniform. It integrated smoothly into our conjugation workflow with no observable issues.
19/9/2020
— Dr. Isabelle Fournier, ADC Development Lead (France)
MA-PEG4-VA-PBD showed excellent stability in our formulation tests. We appreciated the clear documentation provided.
12/8/2021
— Mr. Daniel Carter, Chemist (UK)
Working with BOC Sciences on MA-PEG4-VA-PBD was seamless. The linker’s reactivity was consistent across multiple trials.
7/2/2023
— Dr. Sophie Klein, Pharmaceutical Researcher (Netherlands)
High-quality MA-PEG4-VA-PBD that met all our project requirements. Customer support was responsive and knowledgeable.
— Prof. Michael Brown, Medicinal Chemist (Canada)
MA-PEG4-VA-PBD performed reliably in our preclinical ADC conjugations. Documentation and handling guidance were excellent.
28/11/2020
MA-PEG4-VA-PBD
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MA-PEG4-VA-PBD
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