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-W800617
    NH2-PEG1-Val-Cit-PAB-OH
    NH2-PEG1-Val-Cit-PAB-OH is a cleavable ADC linker intermediate featuring a primary amine, a hydrophilic PEG spacer, a Val-Cit dipeptide, and a PAB group. The benzylic alcohol on the PAB can be used to attach with reactive groups such as PNP for conjugation with drug payloads. The primary amine is free to perform a wide variety of reactions such as coupling with carboxylic acids, reductive aminations with ketones or aldehydes, or other more specialized uses such as in SNAr reactions or heterocyclic chemistry. The Val-Cit dipeptide is cleaved by cellular proteases within the cell to allow for efficient payload delivery via an elimination mechanism within the PAB structure.
    NH2-PEG1-Val-Cit-PAB-OH
  • HY-151703
    Boc-D-Lys(N3)-OH
    Boc-D-Lys(N3)-OH is a Boc-protected amino acid derivative, can be used as a click chemistry reagent and an intermediate for synthesis of linkers. 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.
    Boc-D-Lys(N3)-OH
  • HY-41062
    N-Boc-MeVal
    N-Boc-MeVal is an ADC linker with BOC protecting group.
    N-Boc-MeVal
  • HY-151763
    Boc-L-Aza-OH (CHA)
    Boc-L-Aza-OH CHA is a click chemistry reagent containing an azide group. 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.
    Boc-L-Aza-OH (CHA)
  • HY-156319
    BCN-exo-PEG2-NH2
    BCN-exo-PEG2-NH2 is an ADC Linker containing 2 PEG units. BCN-exo-PEG2-NH2 contains the lyophilic bidentate macrocyclic ligand BCN, which can further synthesize macrocyclic complexes. In click chemistry, BCN reacts with molecules containing azide groups to form stable triazoles in the absence of catalysts.
    BCN-exo-PEG2-NH2
  • HY-W800619
    NH2-PEG4-Val-Cit-PAB-OH
    NH2-PEG4-Val-Cit-PAB-OH is a cleavable ADC linker featuring a primary amine, a hydrophilic PEG spacer, a Val-Cit dipeptide, and a PAB group. The benzylic alcohol on the PAB can be used to attach with reactive groups such as PNP for conjugation with drug payloads. The primary amine is free to perform a wide variety of reactions such as coupling with carboxylic acids, reductive aminations with ketones or aldehydes, or other more specialized uses such as in SNAr reactions or heterocyclic chemistry. The Val-Cit dipeptide is cleaved by cellular proteases within the cell to allow for efficient payload delivery via an elimination mechanism within the PAB structure.
    NH2-PEG4-Val-Cit-PAB-OH
  • HY-156323
    BCN-exo-PEG4-NHS
    BCN-exo-PEG4-NHS is an ADC Linker containing 4 PEG units. BCN-exo-PEG4-NHS contains the lyophilic bidentate macrocyclic ligand BCN, which allows for further synthesis of macrocyclic complexes. In click chemistry, BCN reacts with molecules containing azide groups to form stable triazoles in the absence of catalysts.
    BCN-exo-PEG4-NHS
  • HY-151725
    N3-Pen-Dtpp
    N3-Pen-Dtpp is a click chemistry reagent containing an azide group. 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-Pen-Dtpp
  • HY-151841
    N3-L-Lys(Boc)-OH
    N3-L-Lys(Boc)-OH is a click chemistry reagent containing an azide group. N3-L-Lys(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-Lys(Boc)-OH
  • HY-151859A
    N3-Gly-Gly-OH (DCHA)
    N3-Gly-Gly-OH (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.
    N3-Gly-Gly-OH (DCHA)
  • HY-151699
    6-Azidohexanoyl-Val-Cit-PAB-PNP
    6-Azidohexanoyl-Val-Cit-PAB-PNP is a click chemistry reagent that can be used to synthesis 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.
    6-Azidohexanoyl-Val-Cit-PAB-PNP
  • HY-400356
    Glucocorticoid receptor agonist-1 phosphate Gly-Glu TFA
    98.84%
    Glucocorticoid receptor agonist-1 phosphate Gly-Glu (TFA) is a cleavable linker, that can be used to synthesize Antibody-Drug Conjugates (ADCs).
    Glucocorticoid receptor agonist-1 phosphate Gly-Glu TFA
  • HY-151788
    MeO-PEG-alkyne (MW 750Da)
    MeO-PEG-alkyne (MW 750Da) is a click chemistry reagent containing an alkyne group. 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.
    MeO-PEG-alkyne (MW 750Da)
  • HY-W099352
    (2R,3S)-3-(tert-Butoxy)-2-(4-ethyl-2,3-dioxopiperazine-1-carboxamido)butanoic acid
    (2R,3S)-3-(tert-Butoxy)-2-(4-ethyl-2,3-dioxopiperazine-1-carboxamido)butanoic acid is an ADC linker.
    (2R,3S)-3-(tert-Butoxy)-2-(4-ethyl-2,3-dioxopiperazine-1-carboxamido)butanoic acid
  • HY-151838
    (2S,3S)-H-Abu(3-N3)-OH hydrochloride
    (2S,3S)-H-Abu(3-N3)-OH (hydrochloride) is a click chemistry reagent containing an azide group. (2S,3S)-H-Abu(3-N3)-OH (hydrochloride) 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.
    (2S,3S)-H-Abu(3-N3)-OH hydrochloride
  • HY-151730
    (Me)Tz-butanoic acid
    (Me)Tz-butanoic acid is a click chemistry reagent containing an azide. (Me)Tz-butanoic acid is tetrazine linker for conjugation via Diels-Alder-reaction, i.e. copper-free Click reaction with dienophiles. (Me)Tz-butanoic acid is a click chemistry reagent, it contains a Tetrazine group that can undergo an inverse electron demand Diels-Alder reaction (iEDDA) with molecules containing TCO groups.
    (Me)Tz-butanoic acid
  • HY-151693A
    H-L-Tyr(2-azidoethyl)-OH
    H-L-Tyr(2-azidoethyl)-OH is a unnatural Tyrosine derivative. H-L-Tyr(2-azidoethyl)-OH is a click chemistry reagent containing an azide group. 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-L-Tyr(2-azidoethyl)-OH
  • HY-W250992
    Boc-L-Lys(N3)-OH (CHA)
    Boc-L-Lys(N3)-OH CHA is a click chemistry reagent containing an 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.
    Boc-L-Lys(N3)-OH (CHA)
  • HY-151707
    DACN(Tos,Ns)
    DACN(Tos,Ns) is a click chemistry reagent containing an cyclic alkyne group.
    DACN(Tos,Ns)
  • HY-140025
    Propargyl-PEG4-CH2CO2-NHS
    Propargyl-PEG4-CH2CO2-NHS (compound P-7) is a PEG derivative containing a propargyl group and an NHS group. Propargyl-PEG4-CH2CO2-NHS is an ADC linker used in the synthesis of antibody-drug conjugates (ADCs). Propargyl-PEG4-CH2CO2-NHS 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-CH2CO2-NHS

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