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 |
---|---|---|---|---|
V54547 | 4-Azido-2,3,5,6-tetrafluorobenzoic acid (N3-TFBA) | 122590-77-6 | 4-Azido-2,3,5,6-tetrafluorobenzoic Acid (N3-TFBA) is an azide-bearing reagent for click chemistry. | |
V54655 | 4-Azidobenzyl alcohol | 31499-54-4 | 4-Azidobenzyl alcohol is a dot chemical reagent containing an Azide (N3) moiety. | |
V54573 | 4-N3Pfp-NHSester | 126695-58-7 | 4-N3Pfp-NHS ester is a non-cleavable (non-degradable) ADC linker used for the synthesis of antibody-conjugated active molecules (ADCs). | |
V54695 | 4-Pentynoyl-Val-Ala-PAB | 1956294-75-9 | 4-Pentynoyl-Val-Ala-PAB is an azide group-containing click chemistry reagent. | |
V51224 | 4-Pentynoyl-Val-Ala-PAB-PNP | 1956294-76-0 | 4-Pentynoyl-Val-Ala-PAB-PNP is a cleavable (degradable) ADC (Antibody-drug conjugate) linker that has been used to synthesize cryptomycin conjugates. | |
V76156 | 4-Succinimidyl-oxycarbonyl-α-(2-pyridyldithio)toluene | 160854-54-6 | 4-Succinimidyl-oxycarbonyl-α-(2-pyridyldithio)toluene is a non-cleavable (non-degradable) ADC linker that may be utilized to prepare active antibody conjugated molecules (ADC). | |
V54569 | 6-Azido-D-lysine | 1418009-93-4 | 6-Azido-D-lysine is a dot chemical reagent containing azide. | |
V54586 | 6-Azido-D-lysine hydrochloride | 2098497-01-7 | 6-Azido-D-lysine HCl is a chemical reagent containing azide. | |
V52741 | 6-Azido-hexylamine | 349553-73-7 | 6-Azido-hexylamine is a cleavable (degradable) ADC (Antibody-drug conjugate) linker that may be utilized to prepare active antibody conjugated molecules (ADC). | |
V54632 | 6-Azidohexanoyl-Val-Cit-PAB | 1613321-02-0 | 6-Azidohexanoyl-Val-Cit-PAB is a reagent for click chemistry that may be utilized to prepare vaccines. | |
V54680 | 6-Azidohexanoyl-Val-Cit-PAB-PNP | 1613321-01-9 | 6-Azidohexanoyl-Val-Cit-PAB-PNP is a reagent for click chemistry that may be utilized to prepare vaccines. | |
V54492 | 6-O-Propynyl-2'-deoxyguanosine | 1640051-47-3 | 6-O-Propynyl-2'-deoxyguanosine is a reagent for click chemistry containing an alkyne group. | |
V54670 | 8-Azido-octanoyl-OSu | 2576471-56-0 | 8-Azido-octanoyl-OSu is a reagent for click chemistry bearing an azide (N3) moiety. | |
V76108 | AcBut (4-(4-Acetyl-phenoxy)-butyric acid) | 65623-82-7 | AcBut is a degradable Ozogamicin linker used to synthesize Ozogamicin, a drug-linker conjugate for ADC. | |
V54611 | Acid-C3-SSPy | 250266-79-6 | Acid-C3-SSPy is a cleavable DBA-DM4 linker used in the preparation /synthesis of DBA-DM4. | |
V53384 | AcLys-PABC-VC-Aur0101 intermediate-1 | 1609108-48-6 | AcLys-PABC-VC-Aur0101 intermediate-1 is a cleavable (degradable) ADC (Antibody-drug conjugate) linker that may be utilized to prepare antibody-conjugated active molecules (ADC). | |
V52862 | AEEA-AEEA | 1143516-05-5 | AEEA-AEEA is a cleavable ADC (Antibody-drug conjugate) linker, used to synthesize ADCs (antibody-drug conjugates). | |
V54584 | Ala-Ala-Asn-PAB | 2149584-00-7 | Ala-Ala-Asn-PAB is a protein-degradable (cleavable) ADC linker widely used in Antibody-drug conjugates (ADCs). | |
V79914 | Ala-Ala-Asn-PAB TFA | Ala-Ala-Asn-PAB TFA is a widely used protein-degradable (cleavable) ADC linker for Antibody-drug conjugates (ADCs). | ||
V80107 | Ala-CO-amide-C4-Boc | Ala-CO-amide-C4-Boc is a cleavable (degradable) ADC (Antibody-drug conjugate) linker that may be utilized to prepare Antibody-drug conjugates (ADC). |