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 |
|---|---|---|---|---|
|
V52625 | Cyclooctyne-O-amido-PEG2-PFP ester | 2101206-61-3 | Cyclooctyne-O-amido-PEG2-PFP ester is a non-cleavable (non-degradable) ADC linker containing 2 PEG (polyethylene glycol) units, which may be utilized to prepare active ADC molecules. |
|
V52624 | Cyclooctyne-O-amido-PEG3-PFP ester | 2101206-33-9 | Cyclooctyne-O-amido-PEG3-PFP ester is a non-cleavable (non-degradable) ADC linker containing 3 PEG (polyethylene glycol) units, which may be utilized to prepare active ADC molecules. |
|
V78955 | Cyclooctyne-O-amido-PEG4-PFP ester | Cyclooctyne-O-amido-PEG4-PFP ester is a non-cleavable (non-degradable) ADC linker containing 4 PEG (polyethylene glycol) units, which may be utilized to prepare active ADC molecules. | |
|
V52447 | Cyclooctyne-O-NHS ester | 1425803-45-7 | Cyclooctyne-O-NHS ester is a cleavable ADC bridge used for the synthesis of antibody active molecule conjugates (ADCs). |
|
V52444 | Cyclooctyne-O-PFP ester | 886209-60-5 | Cyclooctyne-O-PFP ester is a cleavable ADC bridge used for the synthesis of antibody active molecule conjugates (ADCs). |
|
V40168 | D-Proline, 4-hydroxy-, methyl ester hydrochloride | 114676-59-4 | D-Proline, 4-hydroxy-, methyl ester ( HCl) is a non-cleavable (non-degradable) ADC linker used to synthesize active antibody conjugated molecules (ADCs). |
|
V54668 | DACN(Ms) hydrochloride | 2331322-16-6 | DACN(Ms) ( HCl) (compound 1ba) is a reagent for click chemistry containing cyclononyne. |
|
V54675 | DACN(Ms,Ns) | 2411082-25-0 | DACN(Ms,Ns) is a reagent for click chemistry containing a cycloalkyne group. |
|
V54692 | DACN(Tos) hydrochloride | 2331322-18-8 | DACN(Tos) HCl is a reagent for click chemistry containing a cycloalkyne group. |
|
V54689 | DACN(Tos,Mal) | 2411082-28-3 | DACN(Tos,Mal) is a reagent for click chemistry containing azide. |
|
V54714 | DACN(Tos,Ns) | 1797508-58-7 | DACN(Tos,Ns) is a reagent for click chemistry containing a cycloalkyne group. |
|
V54657 | DACN(Tos,Suc-NHS) | 2411082-26-1 | DACN(Tos,Suc-NHS) is a reagent for click chemistry containing a cycloalkyne group |
|
V54650 | DACN(Tos,Suc-OH) | 2109751-68-8 | DACN(Tos,Suc-OH) is a reagent for click chemistry containing a cycloalkyne group. |
|
V54713 | DACN(Tos2) | 1797508-57-6 | DACN(Tos2) is a reagent for click chemistry containing a cycloalkyne group. |
|
V54688 | DACN(Tos2,6-OH) | 2109751-74-6 | DACN(Tos2,6-OH) is an azide-bearinging reagent for click chemistry . |
|
V53400 | Dap-NE hydrochloride | 2019182-02-4 | Dap-NE HCl is a dipeptide HCl and a cleavable ADC (Antibody-drug conjugate) linker. |
|
V54699 | DAPOA | 2389064-43-9 | DAPOA is an azide-bearing reagent for click chemistry. |
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V80041 | DAPOA (DCHA) | DAPOA DCHA is a reagent for click chemistry containing azide. | |
|
V79020 | DBCO-(PEG2-Val-Cit-PAB)2 | DBCO-(PEG2-Val-Cit-PAB)2 is a cleavable ADC (Antibody-drug conjugate) linker containing 4 PEG (polyethylene glycol) units, which may be utilized to prepare active ADC molecules. | |
|
V19218 | DBCO-acid | 1353016-70-2 | DBCO-acid is a non-activated and cleavable building block and ADC linker that can add minimal spacer to modified molecules such as in the synthesis of ADC linker DBCO-NHS ester. |
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