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CAS No.: 2259318-52-8
Cat No.: BADC-00737
4.5 
MA-PEG4-VC-PAB-DMEA-PNU159682 is a drug-linker conjugate for ADC by using PNU159682 (a potent DNA topoisomerase II inhibitor), linked via MA-PEG4-VC-PAB-DMEA.
Structure of 2259318-52-8
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MA-PEG4-VC-PAB-DMEA-PNU159682 is a highly potent ADC Cytotoxin with Linker, composed of the DNA-interacting payload PNU159682 connected via a protease-cleavable VC-PAB ADC Linker and a PEG4 spacer. This design ensures that the ADC payload remains stable in systemic circulation and is released specifically within antigen-expressing tumor cells. As a defined ADC Cytotoxin, it delivers PNU159682 efficiently, facilitating DNA alkylation and crosslinking that induce apoptosis while maintaining controlled intracellular release through the cleavable linker.
The cytotoxic mechanism of MA-PEG4-VC-PAB-DMEA-PNU159682 relies on antibody-mediated binding to tumor-associated antigens and internalization into malignant cells. Inside lysosomes, the VC-PAB linker is cleaved by proteases, releasing PNU159682. This targeted release ensures that the ADC payload exerts its DNA crosslinking activity specifically in tumor cells, achieving potent cytotoxic effects with minimal systemic exposure. The PEG4 spacer improves solubility and flexibility, supporting efficient conjugation and functional activity.
MA-PEG4-VC-PAB-DMEA-PNU159682 features a maleimide attachment site for stable conjugation to monoclonal antibodies, producing homogeneous ADC Cytotoxins with Linker. The cleavable linker and PEG4 spacer enable predictable intracellular payload release and reliable cytotoxic performance. Its chemical properties, including solubility and linker stability, facilitate controlled ADC assembly and consistent delivery of the PNU159682 payload in antigen-positive cells.
Applications of MA-PEG4-VC-PAB-DMEA-PNU159682 are focused on its role as a defined ADC payload-linker combination for constructing homogeneous antibody-drug conjugates. The protease-sensitive VC-PAB linker and PEG4 spacer provide controlled release of PNU159682 within target cells, ensuring reproducible DNA alkylation and cytotoxic activity. This reagent supports precise intracellular delivery in ADC Cytotoxins with Linker, enabling potent and targeted therapeutic effects for oncology applications.
| Catalog | Product Name | CAS | Inquiry |
|---|---|---|---|
| BADC-01417 | MC-VC-PAB-DMEA-PNU159682 | 1178887-17-6 | |
| BADC-01357 | PNU-159682 carboxylic acid | 1204819-92-0 | |
| 121487-74-9 | trans-4-(Aminomethyl)cyclohexanecarboxamide | 121487-74-9 | |
| BADC-01358 | DMEA-PNU-159682 | 1799421-48-9 | |
| BADC-01424 | NH2-VC-PAB-DMEA-PNU159682 | 2227350-96-9 | |
| BADC-01404 | PNU159682-EDA | 2255344-14-8 | |
| BADC-00671 | Mal-C2-Gly3-EDA-PNU-159682 | 2259318-53-9 | |
| BADC-00867 | Mal-Phe-C4-VC-PAB-DMEA-PNU-159682 | 2259318-54-0 | |
| BADC-00762 | DBCO-PEG4-VC-PAB-DMEA-PNU159682 | 2259318-56-2 | |
| BADC-01426 | VA-PAB-DMEA-PNU159682 | 2414872-62-9 |
What is MA-PEG4-VC-PAB-DMEA-PNU159682?
MA-PEG4-VC-PAB-DMEA-PNU159682 is a highly potent PNU-159682 cytotoxic payload designed for ADC applications. It features a maleimide (MA) conjugation site, PEG4-DMEA solubilizer, a valine-citrulline cleavable linker, and a PAB self-immolative spacer to enable controlled release.
10/8/2018
Dear BOC Sciences, how does the valine-citrulline linker release PNU-159682?
The valine-citrulline linker is cleaved by lysosomal proteases in target cells, initiating PAB self-immolation and releasing the active PNU-159682 payload, allowing for precise intracellular cytotoxic activity.
15/8/2021
Dear BOC Sciences, what is the role of PEG4-DMEA in this ADC payload?
PEG4-DMEA enhances water solubility, reduces aggregation, and improves pharmacokinetics of the ADC. It supports higher drug-to-antibody ratios while maintaining systemic stability and effective payload delivery.
21/6/2018
Dear team, could you please explain how MA-PEG4-VC-PAB-DMEA-PNU159682 is conjugated to antibodies?
The maleimide (MA) group reacts with thiol residues on antibody cysteines to form stable thioether linkages. This conjugation ensures precise attachment and preserves antibody functionality during circulation.
4/7/2022
Good afternoon! Could you please explain what research applications are supported by this payload?
This payload is used in ADC optimization, including cytotoxicity profiling, linker evaluation, pharmacokinetics, and preclinical cancer model studies, providing a platform for developing highly potent targeted therapies.
16/6/2021
— Dr. Sofia Müller, ADC Chemist (Germany)
MA-PEG4-VC-PAB-DMEA-PNU159682 performed reliably with high solubility and predictable reactivity in ADC synthesis.
21/6/2018
— Mr. Thomas Peterson, Bioconjugation Specialist (USA)
Excellent batch quality of MA-PEG4-VC-PAB-DMEA-PNU159682 allowed reproducible conjugations across multiple trials.
16/6/2021
— Dr. Helena Fischer, Senior Scientist (Germany)
The linker MA-PEG4-VC-PAB-DMEA-PNU159682 integrated smoothly with our payload, reducing side reactions.
4/7/2022
— Prof. James Clarke, Medicinal Chemistry (UK)
High stability and solubility profile, ideal for preclinical ADC development.
10/8/2018
— Dr. Laura Nielsen, Research Scientist (Denmark)
MA-PEG4-VC-PAB-DMEA-PNU159682 exceeded expectations in purity and consistency.
— Mr. Michael Davis, Chemist (USA)
Reliable linker that supported smooth ADC assembly. Documentation was thorough and accurate.
15/8/2021
MA-PEG4-VC-PAB-DMEA-PNU159682
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MA-PEG4-VC-PAB-DMEA-PNU159682
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