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CAS No.:
Cat No.: BADC-01278
Purity: ≥95%
4.5 
Mal-Phe-C4-Val-Cit-PAB-DMEA is a maleimide-based ADC linker featuring cleavable peptide sequences for enzymatic payload release. Enhances stability and specificity in antibody-drug conjugates for oncology applications.
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Mal-Phe-C4-Val-Cit-PAB-DMEA is a sophisticated bioconjugate reagent used primarily in the development of targeted drug delivery systems, such as antibody-drug conjugates (ADCs) and peptide-drug conjugates (PDCs). The maleimide (Mal) group facilitates specific and efficient conjugation to thiol-containing molecules, such as antibodies or peptides. The Val-Cit (valine-citrulline) sequence functions as a cleavable linker, enabling controlled release of the drug payload in the tumor microenvironment through enzymatic cleavage. The PAB (p-aminobenzyl) group acts as a spacer, improving the overall stability and solubility of the conjugate. The DMEA (dimethylaminoethyl) moiety provides additional solubility and enhances the pharmacokinetics, ensuring prolonged circulation and reduced non-specific binding.
A major application of Mal-Phe-C4-Val-Cit-PAB-DMEA is in the design and development of targeted antibody-drug conjugates (ADCs) for cancer therapy. The compound allows for the covalent attachment of cytotoxic drugs to monoclonal antibodies or targeting peptides. The cleavable linker (Val-Cit) ensures that the payload is released only within the tumor cells, where specific enzymes cleave the linker, triggering the release of the cytotoxic drug. This targeted delivery system reduces the toxic side effects associated with conventional chemotherapy, as the drug is delivered specifically to cancerous tissues, thereby enhancing the therapeutic efficacy. The PEG-based linker and DMEA group further optimize the solubility and stability of the ADC, improving its pharmacokinetic profile.
Mal-Phe-C4-Val-Cit-PAB-DMEA is also widely employed in peptide-drug conjugates (PDCs), offering a tailored approach to targeted cancer therapy. By linking therapeutic agents to targeting peptides, this compound enables specific delivery of the drug to tumor cells. The cleavable Val-Cit linker ensures that the drug is released once the conjugate reaches its target, further enhancing the precision and effectiveness of the therapy. The addition of the DMEA group provides increased solubility and stability in the bloodstream, making the conjugate more efficient in reaching and acting on the target tissue. This makes Mal-Phe-C4-Val-Cit-PAB-DMEA highly effective in personalized cancer treatments, where peptide-based targeting agents play a crucial role in selective drug delivery.
In addition to drug delivery, Mal-Phe-C4-Val-Cit-PAB-DMEA is useful in molecular imaging and diagnostic applications. By attaching imaging agents such as fluorophores or radiolabels to antibodies or peptides, the compound allows for the targeted detection of biomarkers associated with cancer and other diseases. The cleavable Val-Cit linker ensures that the imaging agent is released in the target area, enhancing the accuracy and sensitivity of diagnostic imaging. The solubility-enhancing DMEA group ensures that the conjugate remains stable and effective in vivo, allowing for prolonged detection of disease markers. This application is key in the development of advanced diagnostic tools for precision medicine.
| 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-00849 | Acetylene-linker-Val-Cit-PABC-MMAE | 1411977-95-1 | |
| BADC-01448 | mDPR-Val-Cit-PAB-MMAE | 1491152-26-1 | |
| BADC-00958 | Amino-PEG4-Val-Cit-PAB-MMAE | 1492056-71-9 | |
| BADC-00708 | Val-cit-PAB-OH | 159857-79-1 | |
| BADC-00968 | MC-Val-Cit-PAB | 159857-80-4 | |
| BADC-00501 | Mc-Val-Cit-PABC-PNP | 159857-81-5 | |
| BADC-00364 | Fmoc-Val-Cit-PAB | 159858-22-7 | |
| BADC-01348 | Val-Cit-PAB-MMAE TFA salt | 1608127-32-7 |
What is Mal-Phe-C4-Val-Cit-PAB-DMEA and its application in ADCs?
Mal-Phe-C4-Val-Cit-PAB-DMEA is an enzyme-cleavable maleimide linker for ADCs, combining a Phe-C4-Val-Cit dipeptide sequence with a self-immolative PAB spacer. It allows stable conjugation and selective lysosomal payload release via protease-mediated cleavage.
9/7/2020
Dear BOC Sciences, how does Mal-Phe-C4-Val-Cit-PAB-DMEA control payload release?
The Val-Cit sequence is recognized by lysosomal proteases, triggering cleavage. The PAB spacer then self-immolates to release the free drug, ensuring targeted intracellular delivery while maintaining ADC stability in circulation.
9/7/2022
Dear BOC Sciences, which conjugation strategies are compatible with Mal-Phe-C4-Val-Cit-PAB-DMEA?
The maleimide group enables thiol-specific conjugation with cysteine residues on antibodies. This supports site-specific ADC synthesis with defined drug-antibody ratios, combining enzymatic payload release with controlled conjugation chemistry.
25/12/2016
Dear BOC Sciences, what factors affect the performance of Mal-Phe-C4-Val-Cit-PAB-DMEA in ADCs?
Critical factors include reaction pH, temperature, thiol availability, and payload hydrophobicity. Optimizing these conditions ensures high conjugation efficiency, linker stability in plasma, and predictable intracellular drug release.
24/8/2019
Dear team, what precautions are necessary when storing Mal-Phe-C4-Val-Cit-PAB-DMEA?
Mal-Phe-C4-Val-Cit-PAB-DMEA should be stored in a cool, dry environment, preferably at -20°C, protected from light and moisture. Avoid repeated freeze-thaw cycles. Proper storage preserves the maleimide functionality critical for thiol conjugation in ADC preparation and ensures long-term chemical stability.
8/12/2019
— Dr. Emily Carter, Senior Scientist (USA)
Mal-Phe-C4-Val-Cit-PAB-DMEA linker enabled high-efficiency conjugation with consistent payload release.
25/12/2016
— Prof. David Müller, Medicinal Chemist (Germany)
BOC Sciences delivered Mal-Phe-C4-Val-Cit-PAB-DMEA with excellent purity and batch-to-batch consistency.
8/12/2019
— Dr. Anna Rossi, Bioconjugation Specialist (Italy)
The linker’s design allowed reproducible ADC yields with minimal side reactions.
24/8/2019
— Mr. James Thompson, R&D Manager (UK)
Using Mal-Phe-C4-Val-Cit-PAB-DMEA, we achieved efficient intracellular payload release.
9/7/2020
— Dr. Laura Jensen, ADC Project Lead (Denmark)
Excellent solubility and functional group stability improved workflow efficiency.
— Ms. Sophie Martin, Senior Researcher (France)
The linker consistently performed well in conjugation and enzymatic cleavage assays.
9/7/2022
Mal-Phe-C4-Val-Cit-PAB-DMEA
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Mal-Phe-C4-Val-Cit-PAB-DMEA
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