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PNU159682-EDA-Gly3

  CAS No.:   Cat No.: BADC-00770 4.5  

PNU159682-EDA-Gly3 is a drug-linker conjugate for ADC by using PNU159682 (a potent DNA topoisomerase II inhibitor), linked via EDA-Gly3.

PNU159682-EDA-Gly3

Structure of

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Category
ADC Cytotoxin with Linker
Molecular Formula
C39H48N6O15
Molecular Weight
840.84
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Room temperature, or blue ice upon request.
Storage
-20°C

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

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Synonyms
PNU-159682-EDA-Gly3
Shipping
Room temperature, or blue ice upon request.
Storage
-20°C

PNU159682-EDA-Gly3 is a highly potent ADC Cytotoxin with Linker, consisting of the DNA-crosslinking PNU159682 payload connected via an EDA-Gly3 linker. This design ensures that the ADC payload remains stable during systemic circulation and is released specifically inside antigen-expressing tumor cells. As a defined ADC Cytotoxin, PNU159682-EDA-Gly3 delivers the PNU159682 payload efficiently, facilitating DNA alkylation and crosslinking that induces apoptosis while maintaining controlled intracellular release through the cleavable linker.

The mechanism of PNU159682-EDA-Gly3 relies on antibody-mediated binding to tumor-associated antigens and internalization into malignant cells. Within lysosomes, the EDA-Gly3 linker is cleaved by proteases, releasing PNU159682 directly inside the cell. This selective release ensures that the ADC payload exerts its DNA-crosslinking cytotoxic activity specifically in tumor cells, maintaining potent efficacy while limiting systemic exposure. The Gly3 spacer provides flexibility and improves solubility, supporting effective conjugation and predictable payload activation.

PNU159682-EDA-Gly3 allows stable conjugation to monoclonal antibodies, generating homogeneous ADC Cytotoxins with Linker. The cleavable EDA-Gly3 linker ensures reliable intracellular payload release and consistent cytotoxic performance. Its chemical properties, including solubility, linker stability, and reproducible cleavage kinetics, facilitate controlled ADC assembly and precise intracellular delivery of the PNU159682 payload in antigen-positive cells.

Applications of PNU159682-EDA-Gly3 focus on its role as a defined ADC payload-linker combination for constructing homogeneous antibody-drug conjugates. The protease-sensitive linker provides controlled intracellular release of PNU159682, producing consistent DNA alkylation and cytotoxicity. This reagent delivers potent, targeted effects in ADC Cytotoxins with Linker, supporting precise intracellular payload delivery for oncology-focused ADC development and research.

What is PNU159682-EDA-Gly3?

PNU159682-EDA-Gly3 is a potent cytotoxic payload derived from PNU-159682, designed for ADC conjugation. It features a short ethylenediamine (EDA) linker and a Gly3 peptide for solubility and controlled release in targeted cells.

22/2/2019

Dear team, how does PNU159682-EDA-Gly3 release its payload?

The payload is released through enzymatic cleavage of the Gly3 segment by intracellular proteases after ADC internalization, allowing the PNU-159682 molecule to induce cytotoxicity selectively in target cells.

19/7/2022

Dear team, what are the advantages of the EDA-Gly3 linker?

The EDA-Gly3 linker improves solubility and reduces aggregation, enabling higher drug-to-antibody ratios. It ensures efficient intracellular delivery while maintaining stability in systemic circulation.

13/5/2022

Could you please let me know what types of ADCs can incorporate PNU159682-EDA-Gly3?

PNU159682-EDA-Gly3 can be conjugated to monoclonal antibodies targeting solid tumors or hematologic malignancies. Its high potency allows low dosing and precise cytotoxic delivery in preclinical ADC studies.

25/8/2016

Dear team, what research applications are supported by PNU159682-EDA-Gly3?

It is used in ADC optimization, including cytotoxicity profiling, pharmacokinetic evaluation, and targeted delivery studies, facilitating the development of highly potent and selective oncology therapeutics.

28/8/2022

— Dr. Anna Schultz, ADC Project Leader (Germany)

PNU159682-EDA-Gly3 linker demonstrated excellent batch consistency and solubility for ADC conjugation.

13/5/2022

— Mr. James Wilson, Bioconjugation Specialist (USA)

Smooth integration into payload conjugation workflow; predictable DAR achieved.

28/8/2022

— Dr. Caroline Dupont, Senior Chemist (France)

High-quality PNU159682-EDA-Gly3 supported reproducible ADC production with minimal side reactions.

25/8/2016

— Prof. Richard Evans, Biochemistry Professor (UK)

Reliable linker with excellent documentation and handling guidance.

22/2/2019

— Dr. Laura Nielsen, Research Scientist (Denmark)

Batch-to-batch consistency of PNU159682-EDA-Gly3 ensured smooth preclinical testing.

— Mr. Thomas Reed, ADC Development Chemist (USA)

High solubility and predictable reactivity profile made this linker ideal for ADC synthesis.

19/7/2022

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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