A desirable monoclonal antibody, an effective cytotoxic drug, and a suitable linker make up antibody-drug conjugates (ADCs). A suitable linker between the antibody and the cytotoxic drug creates a clear bridge, enabling the antibody to precisely deliver the cytotoxic drug to tumor sites and deliver it only to tumor cells. In addition to conjugation, the linkers preserve the stability of ADCs during their preparation, storage, and systemic circulation phases.
The linkers found in the ADCs currently undergoing clinical evaluation are primarily divided into two groups: cleavable and noncleavable. Cleavable linkers rely on internal cellular mechanisms to release the toxin, such as cytoplasmic reduction, exposure to acidic conditions in the lysosome, or cleavage by particular cellular proteases. For the release of the cytotoxic molecule with noncleavable linkers, the antibody portion of the ADC must be broken down by proteolytic enzymes while retaining the linker and the amino acid by which it was attached to the antibody.
Based on knowledge of the internalization and breakdown of the antibody-target antigen complex and a comparison of the preclinical in vitro and in vivo activities of conjugates, the choice of linker depends on the target. Additionally, because each molecule has different chemical restrictions and frequently the drug structure lends itself to a particular linker, the choice of a linker is also influenced by the type of cytotoxin used.
Structure | Cat No. | Product Name | CAS No. | Product Description |
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V53062 | DBCO-C3-Acid | 1207355-31-4 | DBCO-C3-Acid is a click chemistry intermediate. |
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V19220 | DBCO-C6-acid | 1425485-72-8 | DBCO-C6-acid, ananalog of DBCO-Acid with an extended 6-carbon atom spacer arm, isa non-cleavable ADC linker used in the synthesis of antibody-drug conjugates (ADCs). |
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V54633 | DBCO-N-bis(PEG4-NHS ester) | 2639395-38-1 | DBCO-N-bis(PEG4-NHSester) is a PEG linker containing two PEG4-NHS esters and a DBCO group. |
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V54551 | DBCO-NHS ester 3 | 1393350-27-0 | DBCO-NHS ester 3 (Compound 12) is a degradable linker used to prepare ADC molecules. |
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V97278 | DBCO-PEG1-OH | 2754384-62-6 | DBCO-PEG2-C2-acid is an ADC linker. |
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V97235 | DBCO-PEG2-C2-acid | 2305845-07-0 | DBCO-PEG2-C2-acid is an ADC linker. |
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V54506 | DBCO-PEG2-DBCO | 2639395-48-3 | DBCO-PEG2-DBCO is a reagent for click chemistry containing a DBCO group and a PEG linker containing two terminal DBCO groups. |
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V54505 | DBCO-PEG2-NHSester | 2585653-12-7 | DBCO-PEG2-NHS ester is a reagent for click chemistry bearing an azide (N3) moiety. |
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V54580 | DBCO-PEG24-acid | 2765066-36-0 | DBCO-PEG24-acid is a reagent for click chemistry. |
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V85470 | DBCO-PEG24-Maleimide | 2924872-84-2 | |
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V54597 | DBCO-PEG24-NHSester | 2765066-38-2 | DBCO-PEG24-NHS ester is a reagent for click chemistry. |
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V101458 | DBCO-PEG3-acid | 2754384-59-1 | DBCO-PEG3-acid is a non-cleavable ADC linker containing three PEG units for the synthesis of antibody conjugates (ADCs). |
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V97452 | DBCO-PEG3-C1-acid | 2249926-65-4 | DBCO-PEG3-C1-acid is an antibody-drug conjugate (ADC) linker used as a reactive handle for strain-promoted azide-alkyne click reactions. |
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V101261 | DBCO-PEG3-NHS ester | 2163772-16-3 | DBCO-PEG3-NHS ester (cpmpd 45) is an ADC linker used in the synthesis of ADC molecules. |
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V76155 | DBCO-PEG3-oxyamine | 2748394-67-2 | DBCO-PEG3-oxyamine is a non-cleavable (non-degradable) ADC linker containing 3 PEG (polyethylene glycol) units, which may be utilized to prepare ADC molecules. |
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V79024 | DBCO-PEG3-oxyamine-Boc hydrochloride | DBCO-PEG3-oxyamine-Boc HCl is an ADC linker. | |
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V76157 | DBCO-PEG4-alkyne | 2741418-16-4 | DBCO-PEG4-alkyne is a non-cleavable (non-degradable) ADC linker containing 4 PEG (polyethylene glycol) units, which may be utilized to prepare ADC molecules. |
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V52730 | DBCO-SS-acid | 2749426-25-1 | DBCO-SS-acid is a cleavable (degradable) ADC (Antibody-drug conjugate) linker that may be utilized to prepare antibody-conjugated active molecules (ADC). |
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V100136 | DeBoc-Cabazitaxel | 1638286-64-2 | DeBoc-Cabazitaxel is an ADC linker. |
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V54679 | DecarboxyBiotin-Alkyne | 887915-53-9 | DecarboxyBiotin-Alkyne is a reagent for click chemistry bearing an azide (N3) moiety. |