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CAS No.: 2055041-39-7
Cat No.: BADC-01042
Purity: >98.0%
4.5 
Mal-PEG4-Val-Cit-PAB-OH is a maleimide-based PEGylated cleavable ADC linker featuring valine-citrulline for enzymatic drug release, enhancing stability and solubility in antibody-drug conjugates.
Structure of 2055041-39-7
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Mal-PEG4-Val-Cit-PAB-OH is a specialized bioconjugation reagent widely used in the development of targeted drug delivery systems, particularly for antibody-drug conjugates (ADCs) and other precision therapeutic approaches. The compound contains a maleimide (Mal) group that facilitates conjugation with thiol-containing biomolecules, such as peptides or antibodies, while the PEG4 spacer enhances solubility, stability, and pharmacokinetics. The Val-Cit-PAB-OH linker, with its enzymatically cleavable bond, allows for controlled drug release, which is triggered by specific proteases present in the tumor microenvironment. This selective release mechanism helps minimize off-target effects and increases the overall efficacy of therapeutic agents.
One of the most prominent applications of Mal-PEG4-Val-Cit-PAB-OH is in the creation of antibody-drug conjugates (ADCs) for cancer therapy. By attaching cytotoxic drugs to antibodies through the maleimide group, the conjugates are able to specifically target tumor cells expressing relevant surface antigens. The PEG4 spacer improves the solubility and circulation time of the conjugate, while the Val-Cit-PAB-OH linker is cleaved by tumor-specific enzymes, releasing the therapeutic payload directly within the tumor. This selective release mechanism enhances the targeted delivery of the drug, increasing its efficacy and reducing systemic toxicity, making ADCs an effective tool in precision oncology.
Another key application of Mal-PEG4-Val-Cit-PAB-OH is in the development of targeted delivery systems for other types of therapeutics, such as small molecule drugs, oligonucleotides, or gene therapies. The PEG4 spacer improves the pharmacokinetics of the conjugate, ensuring better solubility and stability in biological systems. The enzymatically cleavable linker provides controlled release of the therapeutic agent at the target site, offering high precision in treatment. This makes Mal-PEG4-Val-Cit-PAB-OH an ideal candidate for designing advanced drug delivery systems that can selectively release therapeutic agents at disease sites, such as tumors or infected tissues, thereby enhancing treatment efficacy and minimizing side effects.
In addition to its use in drug delivery, Mal-PEG4-Val-Cit-PAB-OH is valuable for protein and peptide conjugation applications in research. The maleimide group allows for the covalent attachment of peptides, proteins, or antibodies to other molecules, while the PEG4 spacer ensures that the conjugated biomolecules remain soluble and stable in solution. The Val-Cit-PAB-OH linker offers the advantage of controlled release, making this compound useful in applications such as proteomics, molecular imaging, and diagnostic assays, where precise control over the release of biomolecules is crucial for accurate detection and analysis.
| Catalog | Product Name | CAS | Inquiry |
|---|---|---|---|
| BADC-01679 | Mal-PEG2-Val-Cit-PABA-PNP | 1345681-52-8 | |
| BADC-00929 | Fmoc-D-Val-Cit-PAB | 1350456-65-3 | |
| BADC-01448 | mDPR-Val-Cit-PAB-MMAE | 1491152-26-1 | |
| BADC-00968 | MC-Val-Cit-PAB | 159857-80-4 | |
| BADC-00364 | Fmoc-Val-Cit-PAB | 159858-22-7 | |
| BADC-01745 | MC-Val-Cit-PAB-NH-C2-NH-Boc | 1616727-22-0 | |
| BADC-00610 | Mc-Val-Cit-PAB-Cl | 1639351-92-0 | |
| BADC-01470 | MC-Val-Cit-PAB-dimethylDNA31 | 1639352-06-9 | |
| BADC-00611 | MC-Val-Cit-PAB-clindamycin | 1639793-13-7 | |
| BADC-00612 | MC-Val-Cit-PAB-Retapamulin | 1639793-15-9 |
What is the application of Mal-PEG4-Val-Cit-PAB-OH in ADCs?
Mal-PEG4-Val-Cit-PAB-OH is a heterobifunctional linker combining maleimide reactivity with a protease-cleavable Val-Cit motif and PEG4 spacer, used for targeted payload delivery in ADCs.
12/8/2020
Dear BOC Sciences, how does the PEG4 spacer benefit ADC performance?
The PEG4 segment provides increased solubility, reduced aggregation, and enhanced pharmacokinetics, while maintaining accessibility of the Val-Cit-PAB cleavage site for enzymatic release.
14/8/2021
Could you inform us which payloads are compatible with Mal-PEG4-Val-Cit-PAB-OH?
The linker is suitable for thiol-reactive payloads, including MMAE and other auristatins, allowing stable conjugation to cysteine residues on antibodies without compromising antibody function.
4/4/2019
Dear BOC Sciences, what are the key considerations when using Mal-PEG4-Val-Cit-PAB-OH in ADC design?
Important factors include maleimide reactivity control, PEG spacer length optimization, evaluation of in vitro and in vivo stability, and assessment of intracellular cleavage efficiency for optimal payload release.
19/6/2022
Dear team, how should Mal-PEG4-Val-Cit-PAB-OH be handled and stored to preserve maleimide functionality?
Mal-PEG4-Val-Cit-PAB-OH should be stored at -20°C in a dry, inert atmosphere and protected from light. Repeated freeze-thaw cycles should be avoided. Aliquoting is recommended to maintain maleimide reactivity, ensuring consistent and efficient conjugation in ADC preparation.
22/9/2019
— Dr. Emily Carter, Senior Scientist (USA)
Mal-PEG4-Val-Cit-PAB-OH linker showed high solubility and consistent batch quality, greatly facilitating our ADC conjugation processes.
4/4/2019
— Prof. David Müller, Medicinal Chemist (Germany)
BOC Sciences delivered Mal-PEG4-Val-Cit-PAB-OH on schedule with excellent purity and documentation.
22/9/2019
— Dr. Anna Rossi, Bioconjugation Specialist (Italy)
Using Mal-PEG4-Val-Cit-PAB-OH, we achieved reproducible conjugation yields with minimal side reactions.
19/6/2022
— Mr. James Thompson, R&D Manager (UK)
The linker’s PEG4 spacer improved payload accessibility and reduced steric hindrance. Very reliable.
12/8/2020
— Dr. Laura Jensen, ADC Project Lead (Denmark)
Excellent solubility and batch consistency made high-throughput ADC screening efficient.
— Ms. Sophie Martin, Senior Researcher (France)
Mal-PEG4-Val-Cit-PAB-OH consistently performed well in intracellular payload release experiments.
15/8/2021
Mal-PEG4-Val-Cit-PAB-OH
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Mal-PEG4-Val-Cit-PAB-OH
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