Mal-PEG1-Val-Cit-PAB-PNP is a maleimide-functionalized protease-cleavable ADC linker designed for targeted intracellular drug release, enhancing specificity and therapeutic index of antibody-drug conjugates.
Structure of 2249935-92-8
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Capabilities & Facilities
Mal-PEG1-Val-Cit-PAB-PNP is a chemical compound used mainly in drug delivery systems to enhance the stability and efficacy of therapeutic agents. Here are some key applications of Mal-PEG1-Val-Cit-PAB-PNP:
Antibody-Drug Conjugates (ADCs): This compound is employed in the development of ADCs, where it provides a stable linkage between antibodies and cytotoxic drugs. By facilitating the targeted delivery of chemotherapy agents directly to cancer cells, it minimizes damage to healthy tissues and enhances therapeutic efficacy. The unique linker chemistry of Mal-PEG1-Val-Cit-PAB-PNP ensures selective drug release within tumor environments.
Bioconjugation: Mal-PEG1-Val-Cit-PAB-PNP is used for bioconjugation to attach functional molecules to proteins, antibodies, or other biomolecules. The maleimide group allows for specific conjugation with thiol groups, creating stable thioether bonds. This application is especially useful in the design of complex biomolecular structures for research, diagnostics, and therapeutic applications.
Nanoparticle Formulation: This compound can be utilized in the formulation of nanoparticle-based delivery systems. By incorporating Mal-PEG1-Val-Cit-PAB-PNP into nanoparticle structures, it enhances the particles’ stability and provides controlled drug release mechanisms. Such formulations are important for delivering drugs across biological barriers and achieving targeted delivery in biomedical applications.
Protease-Sensitive Linker Systems: Mal-PEG1-Val-Cit-PAB-PNP is applied in creating protease-sensitive linker systems for prodrugs. The valine-citrulline (Val-Cit) sequence is cleavable by specific proteases, which are often overexpressed in pathological tissues such as tumors. This characteristic enables the release of active drugs selectively at the disease site, reducing systemic toxicity and improving therapeutic outcomes.
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 function of Mal-PEG1-Val-Cit-PAB-PNP in ADCs?
Mal-PEG1-Val-Cit-PAB-PNP is a cleavable linker used in ADCs, combining a maleimide for thiol coupling, a Val-Cit dipeptide for protease-mediated cleavage, and PAB-PNP for payload release. It allows targeted cytotoxin delivery to tumor cells while remaining stable in circulation.
2/7/2019
We would like to know how the Val-Cit dipeptide enhances ADC specificity.
The Val-Cit sequence is recognized and cleaved by cathepsin B in lysosomes, enabling selective payload release in target cells. This protease-sensitive mechanism improves therapeutic index by reducing off-target toxicity in normal tissues.
16/12/2018
Could you kindly advise what payload types are compatible with Mal-PEG1-Val-Cit-PAB-PNP?
The maleimide group reacts with cysteine residues on antibodies, making this linker suitable for small molecule cytotoxins containing amines or hydroxyl groups. It supports stable conjugation and controlled intracellular release of payloads.
21/2/2017
Good morning! What are the storage requirements for Mal-PEG1-Val-Cit-PAB-PNP?
Store in dry, low-temperature conditions under inert gas to maintain maleimide reactivity and prevent hydrolysis. Protect from moisture and light to preserve linker integrity until conjugation is performed.
27/9/2018
Dear BOC Sciences, what is the recommended method for handling and detecting Mal-PEG1-Val-Cit-PAB-PNP in ADC preparation?
Mal-PEG1-Val-Cit-PAB-PNP should be handled under inert conditions to prevent premature hydrolysis. Detection and monitoring of reaction progress are commonly performed via HPLC or mass spectrometry. Appropriate quenching agents and buffer systems are advised to maintain linker integrity during antibody conjugation.
11/9/2022
— Dr. Laura Bennett, Senior Chemist (USA)
Mal-PEG1-Val-Cit-PAB-PNP offered excellent stability during multi-step ADC linker synthesis. Highly reliable.
21/2/2017
— Mr. Thomas Müller, Biochemist (Germany)
The reagent showed remarkable coupling efficiency and batch consistency.
11/9/2022
— Dr. Emily Clarke, ADC Scientist (UK)
Using Mal-PEG1-Val-Cit-PAB-PNP, we achieved high-purity conjugates with minimal side products.
27/9/2018
— Dr. Antoine Lefevre, Medicinal Chemist (France)
Integration into our linker design workflow was smooth and predictable.
2/7/2019
— Dr. Sarah Johnson, Research Scientist (USA)
The product facilitated novel linker architectures enhancing solubility and stability.
— Dr. Thomas Wilson, ADC Researcher (Germany)
Mal-PEG1-Val-Cit-PAB-PNP was critical in our ADC linker development. The product stability and solubility supported reproducible conjugation results.
16/12/2018
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