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 |
|---|---|---|---|---|
|
V79749 | (2-Pyridyldithio)-PEG6 acid | 2-Pyridyldithio-PEG6 acid is a cleavable ADC (Antibody-drug conjugate) linker containing 6 PEG (polyethylene glycol) units, which may be utilized to prepare active ADC molecules. | |
|
V54727 | (2R,3S)-Fmoc-Abu(3-N3)-OH | 1932349-21-7 | (2R,3S)-Fmoc-Abu(3-N3)-OH is an Azide (N3) moiety-containing click chemistry reagent. |
|
V56382 | (2R,4R)-1-tert-Butyl 2-methyl 4-hydroxypyrrolidine-1,2-dicarboxylate | 114676-69-6 | N-Boc-cis-4-hydroxy-D-proline methyl ester is a non-cleavable (non-degradable) ADC linker and is used for the synthesis of ADCs (antibody-drug conjugates). |
|
V52876 | (2R,4R)-4-Hydroxypyrrolidine-2-carboxylic acid hydrochloride | 77449-94-6 | cis-4-Hydroxy-D-proline ( HCl) is a non-cleavable (non-degradable) ADC linker, used for the synthesis of ADCs (antibody-drug conjugates). |
|
V54637 | (2R,4R)-Boc-D-Pro(4-N3)-OH | 650601-59-5 | (2R,4R)-Boc-D-Pro(4-N3)-OH is a reagent for click chemistry containing an Azide (N3) moiety. |
|
V54548 | (2R,4R)-Fmoc-D-Pro(4-N3)-OH (cis-4-Azido-N-Fmoc-D-proline) | 1378847-51-8 | (2R,4R)-Fmoc-D-Pro(4-N3)-OH (cis-4-Azido-N-Fmoc-D-proline) is a reagent for click chemistry containing an Azide (N3) moiety. |
|
V54722 | (2R,4R)-HD-Pro(4-N3)-OH hydrochloride | 2737202-69-4 | (2R,4R)-HD-Pro(4-N3)-OH (HCl) is a dot chemical reagent containing an Azide (N3) moiety. |
|
V52877 | (2R,4S)-1-(tert-Butoxycarbonyl)-4-hydroxypyrrolidine-2-carboxylic acid | 147266-92-0 | N-tert-Butoxycarbonyl-trans-4-hydroxy-D-proline is a non-cleavable (non-degradable) ADC linker used to synthesize ADCs (antibody-drug conjugates). |
|
V52875 | (2R,4S)-1-tert-Butyl 2-methyl 4-hydroxypyrrolidine-1,2-dicarboxylate | 135042-17-0 | Boc-trans-D-Hyp-OMe is a non-cleavable (non-degradable) ADC linker used to synthesize antibody-drug-conjugates/ADCss (ADCs). |
|
V54522 | (2R,4S)-Boc-D-Pro(4-N3)-OH | 132622-77-6 | (2R,4S)-Boc-D-Pro(4-N3)-OH is an azide-bearing dot chemical reagent. |
|
V79132 | (2R,4S)-Boc-D-Pro(4-N3)-OH (DCHA) | (2R,4S)-Boc-D-Pro(4-N3)-OH DCHA is an azide-bearinging reagent for click chemistry . | |
|
V54717 | (2R,4S)-Fmoc-D-Pro(4-N3)-OH | 2137142-63-1 | (2R,4S)-Fmoc-D-Pro(4-N3)-OH is a reagent for click chemistry containing an Azide (N3) moiety. |
|
V54701 | (2R,4S)-HD-Pro(4-N3)-OH | 2137086-50-9 | (2R,4S)-HD-Pro(4-N3)-OH is a dot chemical reagent containing an Azide (N3) moiety. |
|
V77677 | (2R,4S)-HD-Pro(4-N3)-OH hydrochloride | (2R,4S)-HD-Pro(4-N3)-OH HCl is a reagent for click chemistry bearing an azide (N3) moiety. | |
|
V54700 | (2S)-N3-HABA | 959148-55-1 | (2S)-N3-HABA is a click chemical reagent. |
|
V54509 | (2S)-N3-IsoSer | 1620171-65-4 | (2S)-N3-IsoSer, a reagent for click chemistry, is an azide-bearing chiral α-hydroxypropionic acid. |
|
V77393 | (2S)-N3-IsoSer (DCHA) | (2S)-N3-IsoSer DCHA is a reagent for click chemistry and is an azide-bearing chiral α-hydroxypropionic acid. | |
|
V54559 | (2S,3R)-Fmoc-Abu(3-N3)-OH | 146306-79-8 | (2S,3R)-Fmoc-Abu(3-N3)-OH is an azide-bearing reagent for click chemistry. |
|
V54731 | (2S,3R)-H-Abu(3-N3)-OH hydrochloride | 2737202-63-8 | (2S,3R)-H-Abu(3-N3)-OH (HCl) is a dot chemical reagent containing an Azide (N3) moiety. |
|
V54738 | (2S,3S)-H-Abu(3-N3)-OH hydrochloride | 2737202-68-3 | (2S,3S)-H-Abu(3-N3)-OH (HCl) is a dot chemical reagent containing an Azide (N3) moiety. |
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