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ADC Linker

ADC (antibody-drug conjugate) drugs consist of a monoclonal antibody, a linker and an active drug (payload). By binding monoclonal antibodies to specific antigens on the surface of tumor cells, cytotoxic drugs are delivered to tumor lesions in a targeted manner, significantly improving safety and efficacy compared to traditional chemotherapeutic and biological drugs.

adc-drug.jpg

The linker is a crucial part of the ADC, which determines the drug release mechanism, PK, therapeutic index and safety of the ADC. Linkers can be divided into two categories: cleavable and non-cleavable. Cleavable linkers are sensitive to the intracellular environment and release free effector molecules and antibodies, such as acid cleavage linkers and protease cleavage linkers, through a combination of catabolism and dissociation in the cell. They are usually stable in blood, but rapidly cleave in low pH and protease-rich lysosomal environments, releasing effector molecules. Non-cleavable linkers are a new generation of linkers that have better plasma stability and tolerance than cleavable linkers, thus reducing off-target toxicity and providing a larger therapeutic window.

Polyethylene glycol (PEG) is one of the most widely used linkers in targeted therapies. 

Role of PEG Linker in ADC

  • 1. Increase water solubility. Sacituzumab-govitecan (IMMU-132) improves water solubility by coupling a cleavable maleimide linker with a short PEG unit to SN-38.

  • 2. Increase the DAR (drug-to-antibody ratio) to improve the efficacy of ADC drugs based on low toxicity.

  • 3. Increase the circulating half-life of ADC drugs.

Huateng Pharma is dedicated to being your most reliable partner to provide high-quality PEG linkers to promote the progress of your ADC R&D. PEG Linker is one of the most widely used linkers  in ADCs, which can increase the water solubility, improve the DAR value and increase the cycle half-life of ADCs.

ADC Linkers with molecular weights and functional groups not listed in our online catalog may be available by custom synthesis. Please inquire at sales@huatengusa.com about pricing and availability.

PEG Linkers for ADC Drugs

Catalog No.

Name

Structure

 Purity 

11185

NH2-PEG24-COOH

NH2-PEG24-COOH.gif≥95%

12277

2-((Azido-PEG8-carbamoyl)methoxy)acetic acid

846549-37-9.gif≥95%

10788

Mal-NH-PEG8-COOH

Mal-NH-PEG8-COOH.gif≥95%

 10631

N3-PEG3-SPA

N3-PEG3-NHS.gif≥95%

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