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ADC Linker

ADC Linker

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.

ADC Linker related products

Structure Cat No. Product Name CAS No. Product Description
(2-Pyridyldithio)-PEG6 acid 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.
(2R,3S)-3-(tert-Butoxy)-2-(4-ethyl-2,3-dioxopiperazine-1-carboxamido)butanoic acid V100131 (2R,3S)-3-(tert-Butoxy)-2-(4-ethyl-2,3-dioxopiperazine-1-carboxamido)butanoic acid 79276-23-6 (2R,3S)-3-(tert-Butoxy)-2-(4-ethyl-2,3-dioxopiperazine-1-carboxamide)butanoic acid is an ADC linker.
(2R,3S)-Fmoc-Abu(3-N3)-OH 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.
(2R,4R)-1-tert-Butyl 2-methyl 4-hydroxypyrrolidine-1,2-dicarboxylate 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).
(2R,4R)-4-Hydroxypyrrolidine-2-carboxylic acid hydrochloride 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).
(2R,4R)-Boc-D-Pro(4-N3)-OH 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.
(2R,4R)-Fmoc-D-Pro(4-N3)-OH (cis-4-Azido-N-Fmoc-D-proline) 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.
(2R,4R)-H-D-Pro(4-N3)-OH hydrochloride 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.
(2R,4S)-1-(tert-Butoxycarbonyl)-4-hydroxypyrrolidine-2-carboxylic acid 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).
(2R,4S)-1-tert-Butyl 2-methyl 4-hydroxypyrrolidine-1,2-dicarboxylate 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).
(2R,4S)-Boc-D-Pro(4-N3)-OH 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.
(2R,4S)-Boc-D-Pro(4-N3)-OH (DCHA) 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 .
(2R,4S)-Fmoc-D-Pro(4-N3)-OH 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.
(2R,4S)-H-D-Pro(4-N3)-OH 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.
(2R,4S)-HD-Pro(4-N3)-OH hydrochloride 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.
(2S)-N3-HABA V54700 (2S)-N3-HABA 959148-55-1 (2S)-N3-HABA is a click chemical reagent.
(2S)-N3-IsoSer V54509 (2S)-N3-IsoSer 1620171-65-4 (2S)-N3-IsoSer, a reagent for click chemistry, is an azide-bearing chiral α-hydroxypropionic acid.
(2S)-N3-IsoSer (DCHA) V77393 (2S)-N3-IsoSer (DCHA) (2S)-N3-IsoSer DCHA is a reagent for click chemistry and is an azide-bearing chiral α-hydroxypropionic acid.
(2S,3R)-Fmoc-Abu(3-N3)-OH 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.
(2S,3R)-H-Abu(3-N3)-OH hydrochloride 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.
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