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DBCO-PEG4-VA-PBD

  CAS No.:   Cat No.: BADC-00755 4.5  

DBCO-PEG4-VA-PBD is a drug-linker conjugate for ADC by using PBD (Pyrrolobenzodiazepine dimers, a potent antitumor antibiotic), linked via DBCO-PEG4-VA.

DBCO-PEG4-VA-PBD

Structure of

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ADC Cytotoxin with Linker
Molecular Formula
C80H87N9O16
Molecular Weight
1430.62
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-20°C

* For research and manufacturing use only. We do not sell to patients.

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Room temperature
Storage
-20°C

DBCO-PEG4-VA-PBD is a potent ADC Cytotoxin with Linker, comprising the DNA-crosslinking PBD (pyrrolobenzodiazepine) payload linked via a cleavable VA-PAB ADC Linker and a PEG4 spacer. The construct maintains stability in circulation while enabling selective intracellular release of the ADC payload in antigen-expressing tumor cells. As a defined ADC Cytotoxin, DBCO-PEG4-VA-PBD delivers the PBD payload efficiently, inducing DNA minor-groove crosslinking and apoptosis with predictable intracellular activation.

The mechanism of DBCO-PEG4-VA-PBD involves antibody-mediated binding to tumor-associated antigens and internalization into target cells. Once inside lysosomes, the VA-PAB linker is cleaved by proteases, releasing the PBD payload. This targeted release ensures the ADC payload exerts its DNA-crosslinking cytotoxic activity specifically in tumor cells, maintaining potent efficacy while limiting systemic exposure. The PEG4 spacer enhances solubility and provides flexibility for efficient conjugation.

DBCO-PEG4-VA-PBD supports stable conjugation to antibodies through its DBCO functional group, producing homogeneous ADC Cytotoxins with Linker. The cleavable VA-PAB linker and PEG4 spacer ensure consistent intracellular payload release and reproducible cytotoxic performance. Its chemical properties, including solubility, linker stability, and predictable cleavage, enable reliable ADC assembly and precise intracellular delivery of the PBD payload in antigen-positive cells.

Applications of DBCO-PEG4-VA-PBD focus on its role as a defined ADC payload-linker combination for constructing homogeneous antibody-drug conjugates. The protease-sensitive linker and PEG4 spacer provide controlled intracellular release of PBD, producing consistent DNA crosslinking and cytotoxicity. This reagent delivers potent, targeted effects in ADC Cytotoxins with Linker, supporting precise and reliable cytotoxic payload delivery in oncology applications.

What is DBCO-PEG4-VA-PBD?

DBCO-PEG4-VA-PBD is a highly potent pyrrolobenzodiazepine (PBD) dimer payload designed for ADCs. It contains a DBCO conjugation site for click chemistry, a PEG4 solubilizing linker, and a valine-alanine (VA) dipeptide linker coupled to a PBD dimer for controlled release in target cells.

3/9/2020

Could you kindly advise how DBCO-PEG4-VA-PBD releases the PBD dimer?

The valine-alanine linker is cleaved by lysosomal proteases after ADC internalization, triggering self-immolation and releasing the PBD dimer payload. This mechanism ensures potent DNA cross-linking selectively within target cells.

7/7/2019

We are interested in knowing the advantages of using PBD dimers in ADCs.

PBD dimers in DBCO-PEG4-VA-PBD provide high cytotoxic potency at low drug concentrations. This enhances ADC efficacy while minimizing systemic toxicity, making them suitable for targeting both hematologic and solid tumor malignancies.

10/4/2020

May I ask how DBCO-PEG4-VA-PBD is conjugated to antibodies?

The DBCO group allows strain-promoted azide-alkyne cycloaddition (SPAAC) with azide-modified antibodies, enabling site-specific and stable conjugation without affecting antibody binding or pharmacokinetics.

5/4/2022

Good morning! What is the primary application of DBCO-PEG4-VA-PBD in research?

DBCO-PEG4-VA-PBD is used in preclinical ADC studies to optimize payload delivery, assess cytotoxicity, evaluate linker stability, and develop highly potent targeted therapies in oncology models.

13/9/2020

— Dr. Emily Thompson, Senior Scientist (USA)

DBCO-PEG4-VA-PBD linker consistently delivered high-quality conjugates with predictable DAR.

10/4/2020

— Prof. Lucas Meyer, Biochemist (Germany)

Excellent stability and reactivity allowed seamless ADC conjugation.

13/9/2020

— Dr. Isabelle Fournier, ADC Research Lead (France)

DBCO-PEG4-VA-PBD integrated smoothly into workflow; minimal side reactions observed.

5/4/2022

— Mr. Daniel Carter, Chemist (UK)

High-purity linker with consistent batch quality, facilitating reliable preclinical studies.

3/9/2020

— Dr. Sophie Klein, Pharmaceutical Researcher (Netherlands)

DBCO-PEG4-VA-PBD’s solubility and handling made conjugation experiments efficient and reproducible.

— Prof. Michael Brown, Medicinal Chemist (Canada)

Reliable ADC assembly with minimal troubleshooting using DBCO-PEG4-VA-PBD.

7/7/2019

The molarity calculator equation

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

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