2. Antibody-drug Conjugate/ADC Related
  3. ADC Linker

ADC 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.

ADC Linker Related Products (1060):

Cat. No. Product Name Effect Purity
  • HY-W019543
    DSS Crosslinker
    DSS Crosslinker is a non-cleavable ADC linker used in the synthesis of antibody-drug conjugates (ADCs)[1].
  • HY-20336
    Mc-Val-Cit-PABC-PNP
    Mc-Val-Cit-PABC-PNP is a cathepsin cleavable linker for antibody-drug conjugates (ADCs) which couples the antibody element to the effecting compound. Mc-Val-Cit-PABC-PNP can be used in the synthesis of ADCs[1][2].
  • HY-42973
    DBCO-NHS ester 99.53%
    DBCO-NHS ester is a cleavable ADC linker used in the synthesis of antibody-drug conjugates (ADCs)[1]. DBCO-NHS ester is a click chemistry reagent, it contains a DBCO group that can undergo strain-promoted alkyne-azide cycloaddition (SPAAC) with molecules containing Azide groups.
  • HY-78738
    MC-Val-Cit-PAB
    MC-Val-Cit-PAB is an intermediate in the synthesis of VcMMAE (HY-15575), which is a Drug-Linker Conjugates for ADC. Monomethyl auristatin E can be used to inhibit Microtubule/Tubulin as ADC Cytotoxin.
  • HY-42360
    SMCC
    SMCC is a protein crosslinker. SMCC-conjugated antigen coupled spleen cells to induce antigen-specific immune responses[1].
  • HY-158135
    Val-Cit-PAB-DEA-COOH
    Val-Cit-PAB-DEA-COOH (compound 17) is an ADC linker that can be used in the synthesis of ADCs[1].
  • HY-160714
    Fmoc-Ala-Ala-Ala-amide-C-O-C-COOH
    Fmoc-Ala-Ala-Ala-amide-C-O-C-COOH (Compound IM-3) is a cleavable ADC linker[1].
  • HY-125933
    Val-Ala-PAB
    Val-Ala-PAB is a cleavable ADC linker that can be used for ADCs synthesis[1].
  • HY-130524
    Amino-PEG4-CH2COOH
    Amino-PEG4-CH2COOH is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs[1]. Amino-PEG4-CH2COOH is also a non-cleavable 4 unit PEG ADC linker used in the synthesis of antibody-drug conjugates (ADCs)[2].
  • HY-126498
    PDEC-NB 99.69%
    PDEC-NB is a disulfide cleavable linker used for the antibody-drug conjugate (ADC).
  • HY-126958
    Biotin-PEG2-acid
    Biotin-PEG2-acid is a non-cleavable 2 unit PEG ADC linker used in the synthesis of antibody-drug conjugates (ADCs). Biotin-PEG2-acid is a PEG-based PROTAC linker can be used in the synthesis of PROTACs.
  • HY-130167
    Fmoc-NH-PEG9-CH2CH2COOH
    Fmoc-NH-PEG9-CH2CH2COOH is a cleavable ADC linker used in the synthesis of antibody-drug conjugates (ADCs). Fmoc-NH-PEG9-CH2CH2COOH is also a PEG-based PROTAC linker that can be used in the synthesis of PROTACs[1].
  • HY-126674
    Mal-Phe-C4-Val-Cit-PAB-DMEA
    Mal-Phe-C4-Val-Cit-PAB-DMEA is a cleavable ADC linker containing a Maleimide group. Mal-Phe-C4-Val-Cit-PAB-DMEA is used for making antibody-drug conjugate.
  • HY-157008
    (S)-TCO-PEG2-Maleimide
    (S)-TCO-PEG2-Maleimide is an ADC linker containing 2 PEG units. (S)-TCO-PEG2-Maleimide can use its own TCO group to perform an inverse electron demand Diels-Alder reaction (iEDDA) with molecules with Tetrazine groups.
  • HY-156307
    Me-Tet-PEG3-Maleimide
    Me-Tet-PEG3-Maleimide is an ADC Linker containing 3 PEG units. Me-Tet-PEG3-Maleimide can utilize its own Tetrazine group to undergo a specific inverse electron demand Diels-Alder reaction (iEDDA) with compounds with TCO groups. Its maleimide group (-Maleimide) degrades in aqueous media and has been used in drug delivery studies.
  • HY-126509
    Mal-amido-PEG10-C2-​NHS ester
    Mal-amido-PEG10-C2-NHS ester is a nonclaevable ADC linker containing a maleimide group and an NHS ester. The NHS ester can be used to label the primary amines (-NH2) of proteins, amine-modified oligonucleotides, and other amine-containing molecules[1][2].
  • HY-151837
    H-L-Phe(4-NH-Poc)-OH hydrochloride
    H-L-Phe(4-NH-Poc)-OH (hydrochloride) is a click chemistry reagent containing an azide group. Used as a modified Phe or Tyr analogue in protein and peptide biosynthesis. Propargyloxycarbonyl, commonly abbreviated as Poc or Pryoc, can either be used as alkyne component for standard Click conjugation or in combination with tetrazine linkers in copper-free Diels-Alder type Click reactions. It also has applications as unusual protecting group for amines, hydroxy functions and as esters. All 3 are stable to neat TFA, but can be cleaved at ambient temperature with Co2(CO)8 in TFA:DCM. Deprotection with other transition metals like palladium have also been reported[1][2]. H-L-Phe(4-NH-Poc)-OH (hydrochloride) is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
  • HY-151783
    DAPOA
    DAPOA is a click chemistry reagent containing an azide group. DAPOA can be used in peptide synthesis as a linker that can be further modified at the azido-groups using Staudinger ligation or click-chemistry[1].
  • HY-136133
    NHS-PEG2-SS-PEG2-NHS
    NHS-PEG2-SS-PEG2-NHS is a cleavable 4 unit PEG ADC linker used in the synthesis of antibody-drug conjugates (ADCs)[1].
  • HY-136051
    Biotin-PEG3-aldehyde
    Biotin-PEG3-aldehyde is a cleavable 3 unit PEG ADC linker used in the synthesis of antibody-drug conjugates (ADCs)[1].