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

Antibody-drug conjugates linker

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.

Cat. No. Product Name Effect Purity Chemical Structure
  • HY-Y0755
    N-Boc-4-hydroxy-L-proline methyl ester
    ≥98.0%
    N-Boc-cis-4-hydroxy-L-proline methyl ester is a non-cleavable ADC linker used in the synthesis of antibody-drug conjugates (ADCs). N-Boc-cis-4-hydroxy-L-proline methyl ester is also a alkyl chain-based PROTAC linker that can be used in the synthesis of PROTACs[2
    N-Boc-4-hydroxy-L-proline methyl ester
  • HY-131158
    DBCO-PEG3-Glu-VC-PABC-MMAF
    DBCO-PEG3-Glu-VC-PABC-MMAF (compound s19b) is a cleavable PEG-based ADC linker that can be used in the synthesis of antibody-drug conjugates (ADCs).
    DBCO-PEG3-Glu-VC-PABC-MMAF
  • HY-129374
    SPDH
    98.57%
    SPDH is a cleavable ADC linker used for diagnosis and treatment of cancer or B cell proliferative diseas.
    SPDH
  • HY-W000423G
    DBCO-amine (GMP)
    DBCO-amine GMP is a GMP grade DBCO-amine (HY-W000423). DBCO-amine is a cleavable ADC linker used in the synthesis of antibody-drug conjugates (ADCs). DBCO-amine is a click chemistry reagent, itcontains a DBCO group that can undergo strain-promoted alkyne-azide cycloaddition (SPAAC) with molecules containing Azide groups.
    DBCO-amine (GMP)
  • HY-136318
    β-D-tetraacetylgalactopyranoside-PEG1-N3
    98.0%
    β-D-tetraacetylgalactopyranoside-PEG1-N3 is a cleavable 1 unit PEG ADC linker used in the synthesis of antibody-drug conjugates (ADCs). β-D-tetraacetylgalactopyranoside-PEG1-N3 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.
    β-D-tetraacetylgalactopyranoside-PEG1-N3
  • HY-156492
    Me-Tet-PEG4-COOH
    98.68%
    Me-Tet-PEG4-COOH is an ADC Linker containing 4 PEG units. Me-Tet-PEG4-COOH can utilize its own Tetrazine group to undergo a specific inverse electron demand Diels-Alder reaction (iEDDA) with compounds with TCO groups.
    Me-Tet-PEG4-COOH
  • HY-141664
    PPA
    99.01%
    PPA is an ADC linker (US20060073528A1). PPA can be used for making antibody-drug conjugate.
    PPA
  • HY-140126
    Bis-Tos-(2-hydroxyethyl disulfide)
    99.51%
    Bis-Tos-(2-hydroxyethyl disulfide) is a cleavable ADC linker used in the synthesis of antibody-drug conjugates (ADCs).
    Bis-Tos-(2-hydroxyethyl disulfide)
  • HY-44235A
    MC-Gly-Gly-D-Phe
    99.38%
    MC-Gly-Gly-D-Phe is a cleavable linker used for sythesis of antibody-drug conjugates (ADC).
    MC-Gly-Gly-D-Phe
  • HY-130923
    BCN-PEG1-Val-Cit-PABC-OH
    BCN-PEG1-Val-Cit-PABC-OH is a cleavable 1 unit PEG ADC linker used in the synthesis of antibody-drug conjugates (ADCs). BCN-PEG1-Val-Cit-PABC-OH is a click chemistry reagent, it contains a BCN group that can undergo strain-promoted alkyne-azide cycloaddition (SPAAC) with molecules containing Azide groups.
    BCN-PEG1-Val-Cit-PABC-OH
  • HY-126519
    PDdEC-NB
    PDdEC-NB is a disulfide cleavable linker used for the antibody-drug conjugate (ADC).
    PDdEC-NB
  • HY-151859
    N3-Gly-Gly-OH
    98.40%
    N3-Gly-Gly-OH is a click chemistry reagent. Click chemistry has great potential for use in binding between nucleic acids, lipids, proteins, and other molecules, and has been used in many research fields because of its beneficial characteristics, including high yield, high specificity, and simplicity. 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-Gly-Gly-OH
  • HY-156317
    BCN-endo-PEG7-maleimide
    BCN-endo-PEG7-maleimide is an ADC Linker containing 7 PEG units. BCN-endo-PEG7-maleimide contains the lyophilic bidentate macrocyclic ligand endo-BCN, which can further synthesize macrocyclic complexes. In click chemistry, endo-BCN can react with molecules containing azide groups to form stable triazoles in the absence of catalysts.
    BCN-endo-PEG7-maleimide
  • HY-151866A
    (S)-N3-HABA (DCHA)
    (S)-N3-HABA (DCHA) is a click chemistry reagent. Click chemistry has great potential for use in binding between nucleic acids, lipids, proteins, and other molecules, and has been used in many research fields because of its beneficial characteristics, including high yield, high specificity, and simplicity. 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.
    (S)-N3-HABA (DCHA)
  • HY-151853A
    N3-L-Leu-OH (BHA)
    N3-L-Leu-OH (BHA) is a click chemistry reagent. Click chemistry has great potential for use in binding between nucleic acids, lipids, proteins, and other molecules, and has been used in many research fields because of its beneficial characteristics, including high yield, high specificity, and simplicity. 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-L-Leu-OH (BHA)
  • HY-151704
    ICG-alkyne
    99.17%
    ICG-alkyne is a click chemistry reagent containing an azide group.
    ICG-alkyne
  • HY-151866
    (2S)-N3-HABA
    (2S)-N3-HABA is a click chemistry reagent. Click chemistry has great potential for use in binding between nucleic acids, lipids, proteins, and other molecules, and has been used in many research fields because of its beneficial characteristics, including high yield, high specificity, and simplicity. 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.
    (2S)-N3-HABA
  • HY-151715
    N3-D-Dap(Fmoc)-OH
    99.87%
    N3-D-Dap(Fmoc)-OH is a click chemistry reagent. N3-D-Dap(Fmoc)-OH can be used as a component for coupling by click reaction and as an orthogonally protected diaminocarboxylic acid derivative. 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-Dap(Fmoc)-OH
  • HY-151717
    N1-Azido-spermine trihydrochloride
    ≥98.0%
    N1-Azido-spermine [Spermine(HHHN3)] trihydrochloride is a click chemistry agent containing azide. 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.
    N1-Azido-spermine trihydrochloride
  • HY-151782A
    H-(Gly)3-Lys(N3)-OH hydrochloride
    99.79%
    H-(Gly)3-Lys(N3)-OH (hydrochloride) is a click chemistry reagent. Click chemistry has great potential for use in binding between nucleic acids, lipids, proteins, and other molecules, and has been used in many research fields because of its beneficial characteristics, including high yield, high specificity, and simplicity. 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.
    H-(Gly)3-Lys(N3)-OH hydrochloride

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