2. Signaling Pathways
  3. Antibody-drug Conjugate/ADC Related
  4. ADC Linker

Antibody-drug conjugates linker

ADC Linker

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Antibody-drug conjugates (ADCs) consist of a desirable monoclonal antibody, an active cytotoxic drug and an appropriate linker. An appropriate linker between the antibody and the cytotoxic drug provides a specific bridge, and thus helps the antibody to selectively deliver the cytotoxic drug to tumor cells and accurately releases the cytotoxic drug at tumor sites. In addition to conjugation, the linkers maintain ADCs’ stability during the preparation and storage stages of the ADCs and during the systemic circulation period.

The ADCs currently undergoing clinical evaluation contain linkers are mostly classified into two categories: cleavable and noncleavable. Cleavable linkers rely on processes inside the cell to liberate the toxin, such as reduction in the cytoplasm, exposure to acidic conditions in the lysosome, or cleavage by specific proteases within the cell. Noncleavable linkers require proteolytic degradation of the antibody portion of the ADC for release of the cytotoxic molecule, which will retain the linker and the amino acid by which it was attached to the antibody.

The selection of linker is target dependent, based on the knowledge of the internalization and degradation of the antibody-target antigen complex, and a preclinical in vitro and in vivo activity comparison of conjugates. Moreover, the choice of a linker is also influenced by which cytotoxin is used, as each molecule has different chemical constraints, and frequently the drug structure lends itself to a specific linker.

ADC Linker Isoform Specific Products:

ADC Linker Isoform Comparison
Cat. No. Product Name Effect Purity Chemical Structure
  • HY-156318
    SCO-PEG3-Maleimide
    SCO-PEG3-Maleimide is a cleavable ADC Linker containing 3 PEG units. SCO-PEG3-Maleimide can be used as a copper-free click chemical reagent for catalyst-free click reactions. Its maleimide group (-Maleimide) degrades in aqueous media and has been used in drug delivery studies.
    SCO-PEG3-Maleimide
  • HY-41063
    N-Boc-N-methyl-D-Valinol
    N-Boc-N-methyl-D-Valinol is an ADC linker with BOC protecting group.
    N-Boc-N-methyl-D-Valinol
  • HY-151744
    N3-TFBA-O2Oc
    N3-TFBA-O2Oc is a click chemistry reagent containing an azide group and an aryl group. Aryl azides are well-known precursors of nitrenes and have been introduced by Fleet et al. as versatile photoaffinity labeling agents to probe biological receptors. This type of compounds has been used as photo-cross linker (λmax=258 nm) in estrogen receptor studies and for direct surface coating of carbon and organic based polymers. N3-TFBA-O2Oc is a click chemistry reagent, it contains an Azide group and can undergo copper-catalyzed azide-alkyne cycloaddition reaction (CuAAc) with molecules containing Alkyne groups. It can also undergo strain-promoted alkyne-azide cycloaddition (SPAAC) reactions with molecules containing DBCO or BCN groups.
    N3-TFBA-O2Oc
  • HY-164731
    Mal-PEG12-DOTA
    Mal-PEG12-DOTA is an ADC linker used in the synthesis of antibody-drug conjugates (ADCs).
    Mal-PEG12-DOTA
  • HY-W800621
    Fmoc-PEG2-Val-Cit-PAB-OH
    Fmoc-PEG2-Val-Cit-PAB-OH is an enzyme-cleavable ADC linker featuring a Boc-protected amine, a hydrophilic PEG spacer, and a Val-Cit-PAB dipeptide. The benzylic alcohol on the PAB can be used to attach with reactive groups such as PNP for conjugation with drug payloads. The Fmoc protecting group may be removed with piperidine to reveal a primary amine for use in coupling reactions to form amides. The Val-Cit-PAB is cleaved by cellular proteases for efficient release of payloads to the cell.
    Fmoc-PEG2-Val-Cit-PAB-OH
  • HY-W591479
    MC-Val-Ala-NHS ester
    MC-Val-Ala-NHS ester is a cleavable ADC linker with a malimide group and an NHS ester group. The Val-Ala linkers can be cleaved by Cathepsin B. Maleimide group is reactive toward thiol groups. MC is reactive with thiol moieties. The NHS ester is able to react specifically and efficiently with amines (e.g. the side chain of lysine residues or aminosilane-coated surfaces) at neutral or slightly basic condition to form a covalent bond.
    MC-Val-Ala-NHS ester
  • HY-151736
    N3-L-Dap(Boc)-OH
    N3-L-Dap(Boc)-OH is a click chemistry reagent containing an azide group. Click chemistry is a powerful chemical reaction with excellent bioorthogonality features: biocompatible, rapid and highly specific in biological environments. N3-L-Dap(Boc)-OH is a click chemistry reagent, it contains an Azide group and can undergo copper-catalyzed azide-alkyne cycloaddition reaction (CuAAc) with molecules containing Alkyne groups. It can also undergo strain-promoted alkyne-azide cycloaddition (SPAAC) reactions with molecules containing DBCO or BCN groups.
    N3-L-Dap(Boc)-OH
  • HY-151714
    Biotin-MeTz
    Biotin-MeTz shiyi is a click chemistry reagent with a terminal methyltetrazine group. Biotin-MeTz shiyi, as a biotin derivative, can be used for the preparation of biotinylated conjugates.
    Biotin-MeTz
  • HY-46572
    Benzyl 2-cyclopropyl-2-hydroxyacetate
    		98.43%
    Benzyl 2-cyclopropyl-2-hydroxyacetate is an intermediate in the synthesis of ADC linker.The linker composed of Benzyl 2-cyclopropyl-2-hydroxyacetate can be coupled to Exatecan (HY-13631) and combined with antibodies (such as antibody hu2F7).
    Benzyl 2-cyclopropyl-2-hydroxyacetate
  • HY-156810
    Fmoc-PEG4-GGFG-CH2-O-CH2-Cbz
    		99.69%
    Fmoc-PEG4-GGFG-CH2-O-CH2-Cbz is a cleavable ADC linker containing 4 units of PEG, which can be used to synthesize active antibody conjugation molecules (ADC).
    Fmoc-PEG4-GGFG-CH2-O-CH2-Cbz
  • HY-164275
    Alkyne-Val-Cit-PAB-OH
    Alkyne-Val-Cit-PAB-OH is a cleavable ADC linker.
    Alkyne-Val-Cit-PAB-OH
  • HY-W108137
    Boc-Gly-Sar-OH
    Boc-Gly-Sar-OH is a cleavable ADC linker.
    Boc-Gly-Sar-OH
  • HY-151783A
    DAPOA (DCHA)
    DAPOA DCHA is a click chemistry reagent containing an azide. DAPOA DCHA can be used in peptide synthesis as a linker that can be further modified at the azido-groups using Staudinger ligation or click-chemistry. This material can be used as a building block for dendrimeric structures. It contains an azide group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing alkyne groups. It can also undergo ring strain-promoted alkyne-azide cycloaddition (SPAAC) with molecules containing DBCO or BCN groups.
    DAPOA (DCHA)
  • HY-151789
    Sulfo DBCO-TFP Ester
    Sulfo DBCO-TFP Ester is a water-soluble, sulfo-containing click chemistry reagent. Sulfo DBCO-TFP Ester enables simple and efficient incorporation of sulfo-DBCO moieties onto amine-containing molecules.
    Sulfo DBCO-TFP Ester
  • HY-151768
    H2N-PEG2-N3 (TosOH)
    H2N-PEG2-N3 (TosOH) is a click chemistry reagent containing an Azide. N3-PEG2-Amine is used as a Click-chemistry linker in various applications. It contains an azide group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing alkyne groups. It can also undergo ring strain-promoted alkyne-azide cycloaddition (SPAAC) with molecules containing DBCO or BCN groups.
    H2N-PEG2-N3 (TosOH)
  • HY-151826
    Fmoc-D-Lys(pentynoyl)-OH
    Fmoc-D-Lys(pentynoyl)-OH is a click chemistry reagent containing an azide group. Used to introduce alkyne functionality into peptides that can be further modified using Click-chemistry.
    Fmoc-D-Lys(pentynoyl)-OH
  • HY-151743
    N3-Cystamine-Suc-OSu
    N3-Cystamine-Suc-OSu is a click chemistry reagent containing an azide group. N3-Cystamine-Suc-OSu can be used for the research of various biochemical. It contains an azide group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing alkyne groups. It can also undergo ring strain-promoted alkyne-azide cycloaddition (SPAAC) with molecules containing DBCO or BCN groups.
    N3-Cystamine-Suc-OSu
  • HY-151829
    Fmoc-L-Asn(EDA-N3)-OH
    Fmoc-L-Asn(EDA-N3)-OH is a click chemistry reagent containing an azide group. This building block is reported in literature for the modification of Amanitin via Click Chemistry. Alpha-Amanitin is the deadliest member of the amatoxin peptide family produced by the death-cap mushroom A. phalloides. It is an orally available, rigid, bicyclic octapeptide and one of the most lethal known natural products (LD50 = 50-100 μg/kg) acting as highly selective allosteric inhibitor of the RNA polymerase II. It contains an azide group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing alkyne groups. It can also undergo ring strain-promoted alkyne-azide cycloaddition (SPAAC) with molecules containing DBCO or BCN groups.
    Fmoc-L-Asn(EDA-N3)-OH
  • HY-W800623
    Fmoc-PEG6-Val-Cit-PAB-OH
    Fmoc-PEG6-Val-Cit-PAB-OH is an enzyme-cleavable ADC linker featuring a Boc-protected amine, a hydrophilic PEG spacer, and a Val-Cit-PAB dipeptide. The benzylic alcohol on the PAB can be used to attach with reactive groups such as PNP for conjugation with drug payloads. The Fmoc protecting group may be removed with piperidine to reveal a primary amine which may be used in coupling reactions to form amides. The Val-Cit-PAB is cleaved by cellular proteases for efficient release of payloads to the cell.
    Fmoc-PEG6-Val-Cit-PAB-OH
  • HY-151764
    N3-D-Orn(Boc)-OH
    N3-D-Orn(Boc)-OH is a Boc-protected pentanoic amino acid derivative, can be used as a click chemistry reagent and has been used to synthesis antibody-drug conjugates (ADC). It contains an azide group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing alkyne groups. It can also undergo ring strain-promoted alkyne-azide cycloaddition (SPAAC) with molecules containing DBCO or BCN groups.
    N3-D-Orn(Boc)-OH
ADC Linker Isoform Comparison

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