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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. Nom du produit Effet Pureté Chemical Structure
  • HY-180563
    ADC 38 drug linker
    ADC 38 drug linker is a drug linker coupling agent used for ADCs, consisting of a CD4 mimic and a linker. ADC 38 drug linker can be used to synthesize antibody-drug conjugates (ADCs), such as ADC 38.
    ADC 38 drug linker
  • HY-164380
    MC-Val-Cit-Gly-exatecan-β-D-glucopyranosiduronic acid
    MC-Val-Cit-Gly-exatecan-β-D-glucopyranosiduronic acid (example 13) is a drug-linker conjugate that consists of a DNA topoisomerase I inhibitor Exatecan (HY-13631) and a linker (HY-180841). MC-Val-Cit-Gly-exatecan-β-D-glucopyranosiduronic acid can be used in synthesis of ADC.
    MC-Val-Cit-Gly-exatecan-β-D-glucopyranosiduronic acid
  • HY-139018
    TLR7/8 agonist 4 hydroxy-PEG10-acid
    TLR7/8 agonist 4 hydroxy-PEG10-acid (compound 9) is a drug-linker conjugates for ADC with potent antitumor activity by using TLR7/8 agonist 4 (HY-139018; a TLR7/8 agonist), linked via the non-cleavable ADC linker hydroxy-PEG10-acid (HY-133307).
    TLR7/8 agonist 4 hydroxy-PEG10-acid
  • HY-160180
    Glucocorticoid receptor agonist-4 Ala-Ala-Mal
    Glucocorticoid receptor agonist-4 Ala-Ala-Mal (Compound Preparation 9) is an anti-human TNFα antibody-glucocorticoid receptor agonist (GC) conjugate. Glucocorticoid receptor agonist-4 Ala-Ala-Mal can be used in the study of autoimmune and inflammatory diseases.
    Glucocorticoid receptor agonist-4 Ala-Ala-Mal
  • HY-161780
    Maleimide-PEG8-Val-Ala-PAB-SNS032
    Maleimide-Val-Ala-PAB-SNS032 is a conjugate of ADC toxin and linker. SNS032 is an inhibitor for CDK, inhibiting the cell cycle at G1/S phase and cell viability of cancer cells. Maleimide-Val-Ala-PAB is a cleavable ADC linker. Maleimide-Val-Ala-PAB-SNS032 can be utilized for the synthesis of ADC molecules.
    Maleimide-PEG8-Val-Ala-PAB-SNS032
  • HY-183253
    DL149
    DL149 is a component of an antibody-drug conjugate (ADC) formed by conjugating the eIF4A inhibitor FD236 (HY-186186) with an ADC linker, and exhibits potential antitumor activity. DL149 can bind to an anti-HER2 antibody to form a complete ADC molecule, which precisely binds to the HER2 receptor on the surface of tumor cells. After internalization into cells, it releases the eIF4A inhibitor payload. DL149 irreversibly blocks the mRNA translation process in tumor cells, thereby inhibiting tumor cell proliferation and inducing their death. DL149 exhibits in vivo antitumor activity in the SK-OV-3 xenograft tumor model, and can be used for the research of HER2-positive solid tumors.
    DL149
  • HY-185492
    MC-cBu-Cit-seco-CBI dimer
    MC-cBu-Cit-seco-CBI dimer (Compound 10) is a conjugate of an ADC drug toxin molecule and a linker, which consists of a DNA alkylating agent connected to a reactive maleimide via a protease-cleavable peptidomimetic linker.
    MC-cBu-Cit-seco-CBI dimer
  • HY-111555
    AmPEG6C2-Aur0131
    AmPEG6C2-Aur0131 is a agent-linker conjugate for ADC (anti-CXCR4 ADC) with potent antitumor activity by using Aur0131 (an auristatin microtubule inhibitor), linked via the non-cleavable linker AmPEG6C2.
    AmPEG6C2-Aur0131
  • HY-128871
    VCP-Eribulin
    VCP-Eribulin is a bioactive molecule-linker conjugate designed for ADCs (Drug-Linker Conjugates for ADC), formed by conjugating an ADC linker (VCP) with Eribulin (HY-13442). Eribulin is a unique microtubule inhibitor exhibiting antitumor activity. VCP-Eribulin can be utilized for antibody conjugation.
    VCP-Eribulin
  • HY-183558
    AV-DL055
    AV-DL055 is a conjugate of the toxin molecule Exatecan (HY-13631) and the linker AV-L03 (HY-183678). AV-DL055 can be used to construct ADCs, such as T-DL055.
    AV-DL055
  • HY-164656
    DOTA-tris(acid)-amido-PEG24-amido-PEG24-DSPE
    DOTA-tris(acid)-amido-PEG24-amido-PEG24-DSPE is a radionuclide conjugate (RDC), which is capable of binding to a radionuclide. RDC has the ability to specifically target biomolecules and can be used in medical imaging or therapy.
    DOTA-tris(acid)-amido-PEG24-amido-PEG24-DSPE
  • HY-158348
    m-PEG8-Lys(Mal)-Val-Ala-PAB-Ph-CO-Dazostinag
    m-PEG8-Lys(Mal)-Val-Ala-PAB-Ph-CO-Dazostinag is a drug-linker conjugate for ADC.
    m-PEG8-Lys(Mal)-Val-Ala-PAB-Ph-CO-Dazostinag
  • HY-183082
    Mal-GFLG-TPP-PPA
    Mal-GFLG-TPP-PPA is a drug-linker conjugate for ADC, and can be used for synthesis of ADCs. Mal-GFLG-TPP-PPA is used in the synthesis of PEG-iPDPA-GFLG-Y-TPPa.
    Mal-GFLG-TPP-PPA
  • HY-183594
    Exatecan-(D-2,4-DHB)-NH2-AA(bPEG8)-Mal
    Exatecan-(D-2,4-DHB)-NH2-AA (bPEG8)-Mal is a linker-payload conjugate. Exatecan-(D-2,4-DHB)-NH2-AA (bPEG8)-Mal contains the linker D-2,4-DHB-NH2-AA(bPEG8)-Mal (HY-183595) and the cytotoxic agent Exatecan (HY-13631), a potent DNA topoisomerase I inhibitor. Exatecan-(D-2,4-DHB)-NH2-AA (bPEG8)-Mal can be utilized for the development of antibody-drug conjugates (ADCs).
    Exatecan-(D-2,4-DHB)-NH2-AA(bPEG8)-Mal
  • HY-160756
    Val-Cit-Exatecan
    Val-Cit-Exatecan is a peptide-linked anti-tumor payload that can be used for the synthesis of antibody-drug conjugates (ADC). Val-Cit-Exatecan consists of DNA TopI inhibitor Exatecan (HY-13631) and a cathepsin-cleavable ADC linker (valine-citrulline). Val-Cit-Exatecan can be used in the research of colorectal cancer, gastric cancer, breast cancer, non-small cell lung cancer, ovarian cancer, head and neck cancer, pancreatic cancer, cervical cancer, and melanoma.
    Val-Cit-Exatecan
  • HY-126689
    Mal-Phe-C4-VC-PAB-DMEA-PNU-159682
    Mal-Phe-C4-VC-PAB-DMEA-PNU-159682, a agent-linker conjugate for ADC, consists the ADC linker Mal-Phe-C4-VC-PAB and a potent ADC cytotoxin DMEA-PNU-159682. DMEA-PNU-159682 includes metabolites of nemorubicin (MMDX) from liver microsomes and ADC cytotoxin PNU-159682.
    Mal-Phe-C4-VC-PAB-DMEA-PNU-159682
  • HY-176455
    ADC-5 drug-linker
    ADC-5 drug-linker (Compound linker-payload 5) is a drug-linker conjugate for ADC with potent anti-tumor activity. ADC-5 drug-linker can be used to synthesize NLRP3 agonist 3 (HY-176452).
    ADC-5 drug-linker
  • HY-171125
    Maytansine derivative M24
    Maytansine derivative M24 is an ADC Drug-Linker Conjugates for ADC that can be used to synthesize ADC REGN5093-M114.
    Maytansine derivative M24
  • HY-177953
    Mal-PEG2-Val-Arg-PABC-OMe-Eribulin
    Mal-PEG2-Val-Arg-PABC-OMe-Eribulin (Compound L-1) is a drug-linker conjugate composed of O-Me Eribulin (HY-159576) and the linker Mal-PEG2-Val-Cit-PAB-OH (HY-130222). Mal-PEG2-Val-Arg-PABC-OMe-Eribulin can be used to synthesize anti-HER3/MET antibody-drug conjugates (ADCs).
    Mal-PEG2-Val-Arg-PABC-OMe-Eribulin
  • HY-177678
    N-(Azido-PEG4)-N-(PEG4-Val-Cit-PAB-MMAE)-N-(PEG4-Val-Cit-PAB-Exatecan)
    N-(Azido-PEG4)-N-(PEG4-Val-Cit-PAB-MMAE)-N-(PEG4-Val-Cit-PAB-Exatecan) is a drug-linker conjugate for ADC (Drug-Linker Conjugate for ADC), consisting of a tubulin polymerization inhibitor MMAE (HY-15162) and a DNA topoisomerase I inhibitor Exatecan (HY-13631), and an ADC linker composition. N-(Azido-PEG4)-N-(PEG4-Val-Cit-PAB-MMAE)-N-(PEG4-Val-Cit-PAB-Exatecan) can be used for synthesis of ADCs and for cancer research.
    N-(Azido-PEG4)-N-(PEG4-Val-Cit-PAB-MMAE)-N-(PEG4-Val-Cit-PAB-Exatecan)
Drug-Linker Conjugates for ADC Isoform Comparison

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