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-135418
    Fmoc-Asp-NH2
    98.49%
    Fmoc-Asp-NH2 is a cleavable ADC linker used in the synthesis of antibody-drug conjugates (ADCs).
    Fmoc-Asp-NH2
  • HY-129942
    S-(1-Hydroxy-2-methylpropan-2-yl) methanesulfonothioate
    S-(1-Hydroxy-2-methylpropan-2-yl) methanesulfonothioate is a glutathione cleavable ADC linker used for the antibody-drug conjugates (ADCs) and refers to the Alkyl-Chain composition. S-(1-Hydroxy-2-methylpropan-2-yl) methanesulfonothioate is the linker portions of the molecules employed for mAb attachment purposes.
    S-(1-Hydroxy-2-methylpropan-2-yl) methanesulfonothioate
  • HY-126516
    Propargyl-PEG4-NHS ester
    Propargyl-PEG4-NHS ester is a nonclaevable 4-unit PEG linker for antibody-agent-conjugation (ADC). Propargyl-PEG4-NHS ester is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
    Propargyl-PEG4-NHS ester
  • HY-133429
    DBCO-PEG3-oxyamine
    98.05%
    DBCO-PEG3-oxyamine is a non-cleavable 3 unit PEG ADC linker used in the synthesis of antibody-drug conjugates (ADCs). DBCO-PEG3-oxyamine is a click chemistry reagent, it contains a DBCO group that can undergo strain-promoted alkyne-azide cycloaddition (SPAAC) with molecules containing Azide groups.
    DBCO-PEG3-oxyamine
  • HY-135975
    MC-Val-Ala-PAB-PNP
    99.51%
    MC-Val-Ala-PAB-PNP is a cleavable ADC linker used in the synthesis of antibody-drug conjugates (ADCs).
    MC-Val-Ala-PAB-PNP
  • HY-130474
    Azido-PEG6-NHS ester
    98.85%
    Azido-PEG6-NHS ester is a cleavable 6 unit PEG ADC linker used in the synthesis of antibody-drug conjugates (ADCs). Azido-PEG6-NHS ester is also a PEG- and Alkyl/ether based PROTAC linker that can be used in the synthesis of PROTACs. Azido-PEG6-NHS ester 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.
    Azido-PEG6-NHS ester
  • HY-W040236
    m-PEG8-Amine
    ≥98.0%
    m-PEG8-Amine is a cleavable ADC linker used in the synthesis of antibody-drug conjugates (ADCs).
    m-PEG8-Amine
  • HY-W010975
    Fmoc-Lys-OH hydrochloride
    99.48%
    Fmoc-Lys-OH hydrochloride is a cleavable ADC linker used in the synthesis of antibody-drug conjugates (ADCs). Fmoc-Lys-OH hydrochloride is also a alkyl chain-based PROTAC linker that can be used in the synthesis of PROTACs.
    Fmoc-Lys-OH hydrochloride
  • HY-W040168
    Amino-PEG2-C2-acid
    ≥98.0%
    Amino-PEG2-C2-acid is a cleavable 3 unit PEG ADC linker used in the synthesis of antibody-drug conjugates (ADCs). Amino-PEG2-C2-acid is also a PEG-based PROTAC linker that can be used in the synthesis of PROTACs.
    Amino-PEG2-C2-acid
  • HY-148462
    Fmoc-Ala-Ala-PAB
    98.86%
    Fmoc-Ala-Ala-PAB is a cleavable ADC linker. Fmoc-Ala-Ala-PAB can be used in the synthesis of antibody-drug conjugates (ADCs).
    Fmoc-Ala-Ala-PAB
  • HY-133439
    BCN-PEG4-NHS ester
    BCN-PEG4-NHS ester is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs. BCN-PEG4-NHS ester 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-PEG4-NHS ester
  • HY-W023121
    Fmoc-Gly-Gly-OH
    99.98%
    Fmoc-Gly-Gly-OH is a cleavable ADC linker used in the synthesis of antibody-drug conjugates (ADCs).
    Fmoc-Gly-Gly-OH
  • HY-130211
    Azido-PEG5-alcohol
    Azido-PEG5-alcohol is a non-cleavable 5 unit PEG ADC linker used in the synthesis of antibody-drug conjugates (ADCs). Azido-PEG5-alcohol is also a PEG-based PROTAC linker that can be used in the synthesis of PROTACs. Azido-PEG5-alcohol 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.
    Azido-PEG5-alcohol
  • HY-136050
    TCO-PEG3-Biotin
    99.90%
    TCO-PEG3-Biotin is a cleavable 3 unit PEG ADC linker used in the synthesis of antibody-drug conjugates (ADCs). TCO-PEG3-Biotin is a click chemistry reagent, it contains a TCO group that can undergo an inverse electron demand Diels-Alder reaction (iEDDA) with molecules containing Tetrazine groups.
    TCO-PEG3-Biotin
  • HY-40141
    1-Boc-azetidine-3-carboxylic acid
    ≥98.0%
    1-Boc-azetidine-3-carboxylic acid is a non-cleavable ADC linker used in the synthesis of antibody-drug conjugates (ADCs). 1-Boc-azetidine-3-carboxylic acid is also a alkyl chain-based PROTAC linker that can be used in the synthesis of PROTACs[2]
    1-Boc-azetidine-3-carboxylic acid
  • HY-138745
    Bis-sulfone-PEG3-Azide
    99.42%
    Bis-sulfone-PEG3-Azide is a cleavable ADC linker used in the synthesis of antibody-drug conjugates (ADCs). Bis-sulfone-PEG3-Azide 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.
    Bis-sulfone-PEG3-Azide
  • HY-W038702
    Boc-Val-Cit-OH
    ≥98.0%
    Boc-Val-Cit-OH is a cleavable ADC linker used in the synthesis of antibody-drug conjugates (ADCs).
    Boc-Val-Cit-OH
  • HY-135971
    endo-BCN-PEG4-acid
    99.27%
    endo-BCN-PEG4-acid is a cleavable 4 unit PEG ADC linker used in the synthesis of antibody-drug conjugates (ADCs). endo-BCN-PEG4-acid is a click chemistry reagent, it contains a BCN group that can undergo strain-promoted alkyne-azide cycloaddition (SPAAC) with molecules containing Azide groups.
    endo-BCN-PEG4-acid
  • HY-40142
    1-N-Boc-3-hydroxyazetidine
    99.03%
    1-N-Boc-3-hydroxyazetidine is a non-cleavable ADC linker used in the synthesis of antibody-drug conjugates (ADCs). 1-N-Boc-3-hydroxyazetidine is also a alkyl chain-based PROTAC linker that can be used in the synthesis of PROTACs
    1-N-Boc-3-hydroxyazetidine
  • HY-151835
    DBCO-PEG24-NHS ester
    DBCO-PEG24-NHS ester is a click chemistry reagent. DBCO-PEG24-NHS ester is a click chemistry PEG reagent containing NHS ester that is able to react specifically and efficiently with primary amines (e.g. the side chain of lysine residues or aminosilane-coated surfaces) at neutral or slightly basic condition to form a covalent bond. The hydrophilic PEG spacer arm improves water solubility and provides a long and flexible connection that minimizes steric hindrance involved with ligation. DBCO is commonly used for copper-free Click Chemistry reactions. Reagent grade, for research use only.
    DBCO-PEG24-NHS ester

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