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 |
|---|---|---|---|---|
|
V54561 | NHPI-PEG3-C2-Pfp ester | 2101206-87-3 | NHPI-PEG3-C2-Pfp ester is a non-degradable linker containing 3 PEG (polyethylene glycol) units, which may be utilized to prepare active ADC molecules. |
|
V54574 | NHPI-PEG4-C2-NHS ester | 1415328-95-8 | NHPI-PEG4-C2-NHS ester, example 40 (WO2014185985A1), is used as a linker for antibody-drug conjugates (ADC). |
|
V54555 | NHPI-PEG4-C2-Pfp ester | 2101206-46-4 | NHPI-PEG4-C2-Pfp ester can be used as a linker for Antibody-drug conjugates (ADC). |
|
V85330 | NHS-Ala-Ala-Asn-active metabolite | 2231135-69-4 | |
|
V76107 | NMS-P945 | 1466546-35-9 | NMS-P945 is an ADC (Antibody-drug conjugate) Linker that may be utilized to prepare antibody drug conjugates (ADC). |
|
V52692 | NO2-SPDB-sulfo | 663598-89-8 | NO2-SPDB-sulfo is a cleavable (degradable) ADC (Antibody-drug conjugate) linker that may be utilized to prepare antibody-conjugated active molecules (ADC). |
|
V52691 | NO2-SPDMV-sulfo | 663599-00-6 | NO2-SPDMV-sulfo is a cleavable (degradable) ADC (Antibody-drug conjugate) linker that may be utilized to prepare active antibody conjugated molecules (ADC). |
|
V54512 | NO2-SPP | 663598-61-6 | NO2-SPP is a degradable linker used to prepare active Antibody-drug conjugates (ADC). |
|
V52690 | NO2-SPP-sulfo | 663598-66-1 | NO2-SPP-sulfo is a cleavable (degradable) ADC (Antibody-drug conjugate) linker that may be utilized to prepare Antibody-drug conjugates (ADC). |
|
V54608 | NO2-SPP-sulfo-Me | 890409-87-7 | NO2-SPP-sulfo-Me is a degradable linker used to prepare active Antibody-drug conjugates (ADC). |
|
V54653 | Norbornene-methyl-NHS | 1986791-87-0 | Norbornene-methyl-NHS is a reagent for click chemistry containing a TCO group. |
|
V54511 | Norborne-NHS | 1888335-48-5 | Norbornene-NHS is a reagent for click chemistry. |
|
V76140 | NSC 135130 | 24164-06-5 | NSC 135130 (compound 11a) is an ADC (Antibody-drug conjugate) Linker with a BOC protecting group that can connect tubulin-targeting inhibitors, may be utilized to prepare drug conjugates. |
|
V53303 | OH-Glu-Val-Cit-PAB-MMAE | 1895916-23-0 | OH-Glu-Val-Cit-PAB-MMAE consists of a cleavable ADC (Antibody-drug conjugate) linker (OH-Glu-Val-Cit-PAB) and a potent tubulin inhibitor (MMAE). |
|
V94103 | pAF-Oxime-PEG4-OH | pAF-Oxime-PEG4-OH is a linker of Opadotina and can be used to prepare antibody-drug conjugates (ADCs). | |
|
V54519 | PDB-Pfp | 2088570-81-2 | PDB-Pfp is a degradable ADC linker used for the synthesis of antibody-conjugated active molecules (ADCs). |
|
V54526 | PDdB-Pfp | 2101206-44-2 | PDdB-Pfp is a cleavable (degradable) ADC (Antibody-drug conjugate) linker designed to target the active molecule TM4SF1 Extracellular Loop 1 (ECL1). |
|
V54501 | PDdEC-NB | 1956318-90-3 | PDdEC-NB is a glutathione cleavable (degradable) cross-linker for antibody conjugation active molecules (ADC). |
|
V52933 | PDEC-NB | 874302-76-8 | PDEC-NB is a disulfide bond cleavable (degradable) cross-linker used for antibody conjugation active molecules (ADC). |
|
V54622 | PDP-C1-Ph-Val-Cit | 1610769-13-5 | PDP-C1-Ph-Val-Cit is a cleavable (degradable) ADC (Antibody-drug conjugate) linker that may be utilized to prepare Antibody-drug conjugates (ADC). |
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