ADC Linker Capabilities of ChemExpress
ChemExpress offers one stop end-to-end CDMO service solutions for Antibodies and ADCs, providing antibodies, payload linkers, conjugates and drug products to biotech & pharma from R&D to commercialization, leveraging an extensive library of ADC payloads and ADC linkers, coupled with years of expertise in synthetic and conjugation chemistry, and supported by a team of over 230 scientists with deep ADC-related expertise, Supported by an advanced synthetic chemistry platform. ChemExpress is dedicated to collaborating with clients to screen and prepare highly customized linker and drug-linker complexes, offers an extensive array of ADC linkers and customized services to support advanced research worldwide, meticulously tailored to advance ADC development. Contact a ChemExpress representative for more information.
ADC Payload-Linker CDMO Integrated Platform
- Preclinical
- Phase I
- Phase II
- Phase III
- Commercial
Payload-Linker Intermediates
XDCConjugation
- Quick Response Fast Delivery
- Full-lifecycle CMC support
- Quality by Design：Continuous Optimization and Improvement
- Rich Experience Dedicated & Reliable
- Cost-effective Stable supply
The Types of ADC Linker
ADC linkers type can be divided into two types according to their cleavage method. cleavable linkers and non-cleavable linkers. Cleavable linkers allow the drug to be separated from the antibody without proteolytic cleavage of the antibody, while non-cleavable linkers require proteolysis of the antibody for the drug to diffuse to its site of action. ChemExpress offers a variety of ADC linker molecules to facilitate antibody-drug conjugate (ADC) development projects.
Cleavable linkers
Cleavable linkers can be further subcategorized as chemically cleavable linkers or enzyme cleavable linkers. Although cleavable linkers are generally preferred over non-cleavable linkers due to their broader range of applicability, they present a greater potential for instability in circulation. Therefore, the success of cleavable linkers hinges on their ability to effectively distinguish between circulatory and target-cell conditions. The poor tumor penetration of large IgG antibodies, combined with any internalization, intracellular trafficking and drug release inefficiencies, leads to the requirement of robust cleavable linker methodologies that maximize delivery of the payloads to cancer cells. Most commonly, cleavable linkers can be severed by acid, reducing agents, or enzymes. Acid-cleavable linkers are most commonly hydrazones; Reductive linkers have most commonly been disulfides; enzyme-cleavable linkers incorporate linkages that are selectively cleaved by enzymes. Enzyme-cleavable linkers most commonly use amides as the linking moieties because of the prevalence of enzymes in organisms that process and cleave amide bonds in proteins.
ChemExpressh offers a wide array of Cleavable linkers such as MAC glucuronide linker-2, Mc-Val-Ala-PAB-PNP, Mc-Val-Cit-PABC-PNP, Fmoc-Val-Cit-PAB-PNP, DBCO-NHS ester etc. To empower our customer's advanced research. These compounds feature great aqueous solubility, and a broad selection of functional groups to choose from.
Non cleavable linkers
Differing from cleavable linkers, non-cleavable linkers have no structural chemical trigger for payload release. Therefore, the active part of a non-cleavable ADC is comprised of an amino acid appendage, a linker and a payload. Non-cleavable linkers are generally unable to exert a bystander effect due to the lack of cell permeability with the charged amino acid appendage. Non-cleavable linkers are mainly effective for the treatment of hematological cancers or tumors with high antigen expression, since over 99% of tumor cells must be killed to achieve remission in a patient.
- [1] Protein & Cell, 2018,9,33-46
- [2] Chem. Soc. Rev., 2019,48,4361-4374
- [3] Pharm Res, 2015,32,3526-3540
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