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-157338
    NHS-Ala-Ala-Asn-active metabolite
    NHS-Ala-Ala-Asn-active metabolite is a cleavable antibody-drug conjugate (ADC) linker for synthesis of kinesin spindle protein (KSP)inhibitor.
    NHS-Ala-Ala-Asn-active metabolite
  • HY-151845
    N3-PhAc-OH
    N3-PhAc-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-PhAc-OH
  • HY-151856
    N3-1,4-cis-CHC-OH
    N3-1,4-cis-CHC-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.
    N3-1,4-cis-CHC-OH
  • HY-151854
    4-(Azidomethyl)benzoic acid
    4-(Azidomethyl)benzoic acid 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.
    4-(Azidomethyl)benzoic acid
  • HY-151766
    DACN(Tos,Suc-OH)
    DACN(Tos,Suc-OH) is a click chemistry reagent containing a cycloalkyne group. The alkyne moiety within the ring has a unique bent structure and high reactivity toward cycloaddition reactions. Such strain-promoted azide-alkyne cycloadditions (SPAAC) using cycloalkynes have served for reliable molecular conjugation in a broad range of fields. The nitrogens are used as connection points for a variety of functional units. DACNs possess high thermal and chemical stability along with comparable click reactivity.
    DACN(Tos,Suc-OH)
  • HY-W800659
    Boc-Gly-Gly-NHS ester
    Chemical
    Boc-Gly-Gly-NHS ester can be used to selectively attach small molecules to specific amino acid residues on proteins, creating conjugates that can be used for a variety of applications in drug discovery and diagnostic assays.
    Boc-Gly-Gly-NHS ester
  • HY-151836
    (2S,3R)-H-Abu(3-N3)-OH hydrochloride
    (2S,3R)-H-Abu(3-N3)-OH (hydrochloride) is a click chemistry reagent containing an azide group. (2S,3R)-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,3R)-H-Abu(3-N3)-OH hydrochloride
  • HY-176478
    PAB-(PEG4-Me)-Cit-Val-PEG2-amide-C2-MC
    PAB-(PEG4-Me)-Cit-Val-PEG2-amide-C2-MC is an ADC linker that can be combined with the TLR7/8 agonist (HY-170770) for the synthesis of a linker-payload conjugate.
    PAB-(PEG4-Me)-Cit-Val-PEG2-amide-C2-MC
  • HY-151752
    Mal-AMCHC-N-Propargylamide
    Mal-AMCHC-N-Propargylamide is a click chemistry reagent containing an azide group. Mal-AMCHC-N-Propargylamide can be a bio-conjugation reagent for antibody-agent-conjugate synthesis using Click-Chemistry.
    Mal-AMCHC-N-Propargylamide
  • HY-141153
    Fmoc-PEG3-Ala-Ala-Asn(Trt)-PAB-PNP
    Fmoc-PEG3-Ala-Ala-Asn(Trt)-PAB-PNP is a cleavable linker for synthesis of antibody-drug conjugates (ADCs).
    Fmoc-PEG3-Ala-Ala-Asn(Trt)-PAB-PNP
  • HY-151781
    Fmoc-L-Dap(Poc)-OH
    Fmoc-L-Dap(Poc)-OH is a click chemistry reagent containing an azide group. Amino acid building block suitable for side chain Click conjugation with standard protocols and together with tetrazine linkers in copper-free Click conjugation (Diels-Alder).
    Fmoc-L-Dap(Poc)-OH
  • HY-W800618
    NH2-PEG3-Val-Cit-PAB-OH
    NH2-PEG3-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-PEG3-Val-Cit-PAB-OH
  • HY-151738
    Fmoc-Aeg(N3)-OH
    Fmoc-Aeg(N3)-OH is a click chemistry reagent containing an Azide. Alkylating the Nitrogen of an amide bond results in peptoid structures, which leads to conformational restrains, like N-methylation and allows backbone derivatisation. Altering cytotoxicity, bacterial cell selectivity and receptor pharmacology through formation of peptoid derivatives have been published for Cilengitide, Piscidin 1, and MC3, MC4 and MC5 receptor agonist. This building block enables design of macrocycles through intermolecular crosslinking or backbone stabilization through intermolecular ring-closure. This compound is a potential building block for the construction of (customized) peptide nucleic acids (PNAs) and for peptoid synthesis. Fmoc-Aeg(N3)-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.
    Fmoc-Aeg(N3)-OH
  • HY-151737
    Z-L-Dbu(N3)-OH
    Z-L-Dbu(N3)-OH is a click chemistry reagent containing an Azide. Z-L-Dbu(N3)-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.
    Z-L-Dbu(N3)-OH
  • HY-151760
    (2R,4S)-H-D-Pro(4-N3)-OH
    (2R,4S)-H-D-Pro(4-N3)-OH is a click chemistry reagent containing an azide group. (2R,4S)-H-D-Pro(4-N3)-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.
    (2R,4S)-H-D-Pro(4-N3)-OH
  • HY-W800837
    t-Boc-N-amido-PEG4-Val-Cit
    t-Boc-N-amido-PEG4-Val-Cit is a protease-cleavable ADC linker featuring a Boc-protected amine, a hydrophilic PEG spacer, and a Val-Cit dipeptide. The Val-Cit dipeptide is cleavable by cell proteases and features a carboxylic acid which is free for coupling reactions with amines to form amides. The Boc can be removed under acidic conditions to reveal a free primary amine, which may be used in a variety of reactions such as coupling or reductive amination.
    t-Boc-N-amido-PEG4-Val-Cit
  • HY-151761
    H-L-Lys(4-N3-Z)-OH hydrochloride
    99.69%
    H-L-Lys(4-N3-Z)-OH hydrochloride is a click chemistry reagent containing an azide group. H-L-Lys(4-N3-Z)-OH hydrochloride contains a lysine-modified azide moiety and as a bioorthogonal ligation handle. H-L-Lys(4-N3-Z)-OH hydrochloride is an infrared probe and a photo-affinity 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.
    H-L-Lys(4-N3-Z)-OH hydrochloride
  • HY-151818
    12-Azido-dodecanoyl-OSu
    12-Azido-dodecanoyl-OSu is a click chemistry reagent containing an azide group. 12-Azido-dodecanoyl-OSu can be used as a hydrophobic bioconjugation linker. 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.
    12-Azido-dodecanoyl-OSu
  • HY-151731
    N3-1,4-trans-CHC-OH
    N3-1,4-trans-CHC-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.
    N3-1,4-trans-CHC-OH
  • 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

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