2. Signaling Pathways
  3. Antibody-drug Conjugate/ADC Related
  4. Drug-Linker Conjugates for ADC

Drug-Linker Conjugates for ADC

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Drug-Linker Conjugates for ADC

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Drug-Linker Conjugates for Antibody Drug Conjugates (ADCs) comprise of an active cytotoxic drug and an appropriate linker. After linked to a monoclonal antibody, those conjugates can be used for making ADCs, which are targeted agents for cancer cells with high selectivity and cytotoxicity.

The drug units in drug-linker conjugates are cytotoxic agents (i.e. ADC cytotoxins or payloads) with antitumor activity and can be classified in DNA damaging agents and tubulin inhibitors. The most commonly used DNA damaging agents in ADCs are Duocarmycins, Pyrrolobenzodiazepines, Camptothecins and Daunorubicins/Doxorubicins, while the popular tubulin inhibitors are Auristatins and Maytansinoids. Besides, there are also many traditional cytotoxic agents can be used in ADCs.

ADC linkers currently undergoing clinical evaluation are mostly classified into two categories: cleavable and noncleavable. Cleavable linkers rely on processes inside the cell to liberate the toxin, and noncleavable linkers require proteolytic degradation of the antibody portion of the ADC for release of the cytotoxic molecule.

Drug-Linker Conjugates for ADC Isoform Specific Products:

Drug-Linker Conjugates for ADC Isoform Comparison
Cat. No. Product Name Effect Purity Chemical Structure
  • HY-169322
    APL-1081
    APL-1081 (Mal-Exo-EVC-MMAE) is part of an antibody-conjugated active molecule (ADC). APL-1081 is conjugated with an ADC linker (peptide Mal-Exo-EEVC) and a potent tubulin polymerization inhibitor, MMAE (HY-15162).
    APL-1081
  • HY-164788
    GGFG-PAB-MMAE
    		99.27%
    GGFG-PAB-MMAE (Comp 58054-1) is a drug-linker conjugate for ADC. GGFG-PAB-MMAE contains the ADC linker (GGFG-PAB) and a potent tubulin polymerization inhibitor MMAE (HY-15162).
    GGFG-PAB-MMAE
  • HY-153962
    SN38-PAB-Lys(MMT)-oxydiacetamide-PEG8-N3
    SN38-PAB-Lys(MMT)-oxydiacetamide-PEG8-N3 is a Drug-Linker Conjugate for ADC. SN38-PAB-Lys(MMT)-oxydiacetamide-PEG8-N3 consists of the anti-cancer agent SN38 (HY-13704) and a linker Lys(MMT)-PAB-oxydiacetamide-PEG8-N3 (HY-131157). SN38-PAB-Lys(MMT)-oxydiacetamide-PEG8-N3 can be used for synthesis of ADCs. SN38-PAB-Lys(MMT)-oxydiacetamide-PEG8-N3 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.
    SN38-PAB-Lys(MMT)-oxydiacetamide-PEG8-N3
  • HY-176415
    Cys-MC-GGFG-Dxd
    Cys-MC-GGFG-Dxd is a conjugate of Cys and Deruxtecan (HY-13631E). Cys-MC-GGFG-Dxd is a linker-toxin building block in antibody-drug conjugates (ADCs) used to link antibody Cys residues to cytotoxic drugs. Cys-MC-GGFG-Dxd can be used in cancer research.
    Cys-MC-GGFG-Dxd
  • HY-160649
    MC-Gly-Gly-Phe-Gly-GABA-Exatecan
    		99.72%
    MC-Gly-Gly-Phe-Gly-GABA-Exatecan is an agent linker conjugate for ADC, with an inhibitor for Topoisomerase Exatecan (HY-13631) with IC50 of 22 μM. MC-Gly-Gly-Phe-Gly-GABA-Exatecan targets various antibodies, exhibits cytotoxic and antitumor efficacy in vitro and in vivo.
    MC-Gly-Gly-Phe-Gly-GABA-Exatecan
  • HY-156687
    GGFG-Eribulin
    GGFG-Eribulin (Compound GGFG) is a Drug-Linker Conjugates for ADC. GGFG-Eribulin consists of the ADC Cytotoxin Eribulin (HY-13442) and a linker. GGFG-Eribulin can be used for synthesis of ADCs.
    GGFG-Eribulin
  • HY-153958
    PDS-MMAE
    		99.76%
    PDS-MMAE (Compound 5’) is a modified MMAE (HY-15162). PDS-MMAE can be used for preparation of neurotensin receptor binding conjugates.
    PDS-MMAE
  • HY-153031A
    Val-Cit-PAB-Exatecan TFA
    		99.73%
    Val-Cit-PAB-Exatecan (Val-Cit-PAB-DX8951) TFA is a agent-linker conjugate for ADC. Val-Cit-PAB-Exatecan TFA is composed of a DNA topoisomerase I DX-8951 (HY-13631) and a cathepsin cleavable ADC linker.
    Val-Cit-PAB-Exatecan TFA
  • HY-128899
    MC-Val-Cit-PAB-Auristatin E
    MC-Val-Cit-PAB-Auristatin E is a agent-linker conjugate for ADC with potent antitumor activity by using Auristatin E (a cytotoxic tubulin modifier), linked via the ADC linker MC-Val-Cit-PAB.
    MC-Val-Cit-PAB-Auristatin E
  • HY-145989A
    Aminobenzenesulfonic auristatin E TFA
    		99.39%
    Aminobenzenesulfonic auristatin E TFA is a agent-linker conjugate for ADC. Aminobenzenesulfonic auristatin E TFA has potent antitumor activity by using Auristatin E (a cytotoxic tubulin modifier), linked via the ADC linker Aminobenzenesulfonic.
    Aminobenzenesulfonic auristatin E TFA
  • HY-148194
    SC239
    		99.97%
    SC239 is a cleavable 2-aminophenyl hemiasterlin agent-linker. SC239 can be as the agent-linker for ADC. SC239 is a click chemistry reagent, it contains a DBCO group that can undergo strain-promoted alkyne-azide cycloaddition (SPAAC) with molecules containing Azide groups.
    SC239
  • HY-147095A
    Val-Ala-PABC-Exatecan trifluoroacetate
    		98.39%
    Val-Ala-PABC-Exatecan trifluoroacetate is a Drug-Linker Conjugates for ADC, consiting of a cleavable Tesirine linker (Val-Ala-PABC) and Exatecan (topoisomerase I inhibitor, HY-13631). Val-Ala-PABC-Exatecan trifluoroacetate can be used for ADC molecues synthesis, such as Mal-PEGn-amide-va-Exatecan.
    Val-Ala-PABC-Exatecan trifluoroacetate
  • HY-153739
    N3-PEG3-VC-PAB-MMAF
    		99.95%
    N3-PEG3-VC-PAB-MMAF (Comp T-88-5) is a drug-linker conjugate containing the ADC linker N3-PEG3-VC-PAB and the tubulin inhibitor MMAF. N3-PEG3-VC-PAB-MMAF 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-PEG3-VC-PAB-MMAF
  • HY-174279
    MCC-AAQ-Exa
    MCC-AAQ-Exa is a drug-linker conjugates for ADC, obtained by condensing the linker with Exatecan (HY-13631) and can be used to prepare antibody-drug conjugates (ADCs). MCC is an ADC linker containing a maleimide fragment.
    MCC-AAQ-Exa
  • HY-128903
    MC-Val-Cit-PAB-carfilzomib iodide
    MC-Val-Cit-PAB-carfilzomib iodide is a agent-linker conjugate for ADC with potent antitumor activity by using carfilzomib (an irreversible proteasome inhibitor), linked via the ADC linker MC-Val-Cit-PAB.
    MC-Val-Cit-PAB-carfilzomib iodide
  • HY-15575S
    VcMMAE-d8
    VcMMAE-d8 is an isotope of VcMMAE (HY-15575). VcMMAE-d8 is a agent-linker conjugate for ADC with potent antitumor activity by using the anti-mitotic agent, monomethyl auristatin E (MMAE, a tubulin inhibitor), linked via the lysosomally cleavable dipeptide, valine-citrulline (vc).
    VcMMAE-d<sub>8</sub>
  • HY-156515
    MC-GGFG-(7ethanol-10NH2-11F-Camptothecin)
    MC-GGFG-(7ethanol-10NH2-11F-Camptothecin) (compound 141) is a drug-linker conjugates for ADC. MC-GGFG-(7ethanol-10NH2-11F-Camptothecin) is a MC-GGFG-(7ethanol-10NH2-11F-Camptothecin) with protease cleavable MC-GGFG linker.
    MC-GGFG-(7ethanol-10NH2-11F-Camptothecin)
  • HY-157407
    Cyclooctyne-O-amido-PEG4-VC-PAB-Gly-Gly-NH-O-CO-Exatecan
    Cyclooctyne-O-amido-PEG4-VC-PAB-Gly-Gly-NH-O-CO-Exatecan is a drug-linker conjugate for ADC (ADC Cytotoxin: Exatecan).
    Cyclooctyne-O-amido-PEG4-VC-PAB-Gly-Gly-NH-O-CO-Exatecan
  • HY-173634
    Mal((3S,3aR,6S,6aR)-Hexahydrofuro[3,2-b]furan-3,6-diamine-PEG12)-β-Glu-PAB-Exatecan
    Mal((3S,3aR,6S,6aR)-Hexahydrofuro[3,2-b]furan-3,6-diamine-PEG12)-β-Glu-PAB-Exatecan (LP1) is a drug-linker conjugate composed of a potent a DNA Topoisomerase I inhibitor Exatecan (HY-13631) and a linker Mal((3S,3aR,6S,6aR)-Hexahydrofuro[3,2-b]furan-3,6-diamine-PEG12)-β-Glu-PAB (HY-173635) to make antibody agent conjugate (ADC), AZD0516 (HY-173639).
    Mal((3S,3aR,6S,6aR)-Hexahydrofuro[3,2-b]furan-3,6-diamine-PEG12)-β-Glu-PAB-Exatecan
  • HY-150402
    MC-Gly-Gly-Phe-Gly-amide-cyclopropanol-amide-Exatecan
    		99.16%
    MC-Gly-Gly-Phe-Gly-amide-cyclopropanol-amide-Exatecan is a pharmaceutical composition containing antibody agent conjugate (ADC). (extracted from patent WO2021190581 Example 1-8).
    MC-Gly-Gly-Phe-Gly-amide-cyclopropanol-amide-Exatecan
Drug-Linker Conjugates for ADC Isoform Comparison

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