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-151746
    N3-Gly-Gly-Gly-OH
    N3-Gly-Gly-Gly-OH is a oligo-Gly click chemistry reagent containing an azide group. Oligo-Gly also has been used as linker to combine different subunits of dimeric or oligomeric proteins or to create artificial multi-domain proteins. By modification into Gly-Gly-Gly-Ser motifs high solubility can be achieved. N3-Gly-Gly-Gly-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-Gly-Gly-Gly-OH
  • HY-W800625
    Boc-PEG4-Val-Cit-PAB-OH
    Boc-PEG4-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 Boc protecting group may be removed with acid 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.
    Boc-PEG4-Val-Cit-PAB-OH
  • HY-160790
    β-Glu-PNP
    β-Glu-PNP is an ADC linker used in the synthesis of antibody-drug conjugates (ADCs).
    β-Glu-PNP
  • HY-49929
    MC-GGFG-NH-CH2-O-CH2-cyclopropane-COOH
    MC-GGFG-NH-CH2-O-CH2-cyclopropane-COOH is an ADC linker that can be combined with the cytotoxic Camptothecin (HY-16560) to form ADC-related drug-linker conjugates (Drug-Linker Conjugates for ADC ).MC-GGFG-NH-CH2-O-CH2-cyclopropane-COOH is conjugated to Camptothecin, which can further bind to the antibody Trastuzumab (HY-P9907) to form Antibody-Drug Conjugates (ADCs).
    MC-GGFG-NH-CH2-O-CH2-cyclopropane-COOH
  • HY-151722
    Boc-D-Orn(N3)-OH (CHA)
    Boc-D-Orn(N3)-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-D-Orn(N3)-OH (CHA)
  • HY-41049
    NSC 135130
    NSC 135130 (compound 11a) is a BOC-protected ADC linker that can be linked to tubulin-targeting inhibitors.Can be used to synthesize drug conjugates.
    NSC 135130
  • HY-151697
    DACN(Tos2)
    DACN(Tos2) is a a click chemistry reagent containing an cycloalkynes group. The alkyne moiety within the ring has a unique bent structure and high reactivity toward cycloaddition reactions. DACN(Tos2) through such strain-promoted azide-alkyne cycloadditions (SPAAC) using cycloalkynes. DACN(Tos2) can be used for the research of molecular conjugation.
    DACN(Tos2)
  • HY-164732
    Fmoc-Lys(DOTA)-OH
    Fmoc-Lys(DOTA)-OH is an ADC linker used in the synthesis of antibody-drug conjugates (ADCs).
    Fmoc-Lys(DOTA)-OH
  • HY-151734
    (2R,3S)-Fmoc-Abu(3-N3)-OH
    (2R,3S)-Fmoc-Abu(3-N3)-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.
    (2R,3S)-Fmoc-Abu(3-N3)-OH
  • HY-151858
    Boc-L-Lys(N3)-OH
    Boc-L-Lys(N3)-OH is a click chemistry reagent containing an azide group. 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.
    Boc-L-Lys(N3)-OH
  • HY-108368A
    Azido-PEG2-CH2COOH (CHA)
    Azido-PEG2-CH2COOH (CHA) is a azido-modified PEG2 acid, can be used as a click chemistry reagent. 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.
    Azido-PEG2-CH2COOH (CHA)
  • HY-151745
    N3-TOTA-Suc
    N3-TOTA-Suc 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-TOTA-Suc 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-TOTA-Suc
  • HY-151709
    N3-L-Cit-OH
    N3-L-Cit-OH is a click chemistry reagent containing an azide group. N3-L-Cit-OH can be used to construct peptidomimetic ADC linkers using Click-chemistry. 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-Cit-OH
  • HY-W108635
    N-[S-Trityl-L-cysteinyl]glycine
    N-[S-Trityl-L-cysteinyl]glycine is a cleavable ADC linker.
    N-[S-Trityl-L-cysteinyl]glycine
  • HY-151839
    (2R,4R)-H-D-Pro(4-N3)-OH hydrochloride
    (2R,4R)-H-D-Pro(4-N3)-OH (hydrochloride) is a click chemistry reagent containing an azide group. (2R,4R)-H-D-Pro(4-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.
    (2R,4R)-H-D-Pro(4-N3)-OH hydrochloride
  • HY-151861
    N3-Aca-Aca-OH
    N3-Aca-Aca-OH is a click chemistry reagent containing an azide group. 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-Aca-Aca-OH
  • HY-151825
    Fmoc-L-Phe(4-NH-Poc)-OH
    Fmoc-L-Phe(4-NH-Poc)-OH is a click chemistry reagent containing an azide group. Used as an orthogonally protected building block in solid-phase peptide synthesis. Poc-group can be further modified using Click-chemistry.
    Fmoc-L-Phe(4-NH-Poc)-OH
  • HY-151865
    (2S,4S)-H-L-Pro(4-N3)-OH
    (2S,4S)-H-L-Pro(4-N3)-OH is a click chemistry reagent containing an azide group. 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,4S)-H-L-Pro(4-N3)-OH
  • HY-151749
    N3-D-Lys(Fmoc)-OH
    N3-D-Lys(Fmoc)-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-D-Lys(Fmoc)-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-D-Lys(Fmoc)-OH
  • HY-151779
    N3-L-Dab(Fmoc)-OH
    N3-L-Dab(Fmoc)-OH is a click chemistry reagent containing an azide group. 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-Dab(Fmoc)-OH
ADC Linker Isoform Comparison

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