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

Drug-Linker Conjugates for ADC

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.

Cat. No. Product Name Effect Purity Chemical Structure
  • HY-157813
    2-MSP-5-HA-GGFG-NH-CH2-O-CH2-CO-Exatecan
    98.27%
    2-MSP-5-HA-GGFG-NH-CH2-O-CH2-CO-Exatecan is a drug-linker conjugates for ADC, consiting of a cleavable linker and Exatecan (HY-13631). 2-MSP-5-HA-GGFG-NH-CH2-O-CH2-CO-Exatecan can be linked to anti-Her3 antibody.
    2-MSP-5-HA-GGFG-NH-CH2-O-CH2-CO-Exatecan
  • HY-126688
    Mal-C2-Gly3-EDA-PNU-159682
    Mal-C2-Gly3-EDA-PNU-159682, a agent-linker conjugate for ADC, consists a cleavable ADC linker Mal-C2-Gly3-EDA and a potent ADC cytotoxin PNU-159682.
    Mal-C2-Gly3-EDA-PNU-159682
  • HY-126494
    DM4-SMCC
    DM4-SMCC is a agent-linker conjugate for ADC with antitumor activity by using DM4 (an antitubulin agent), linked via the non-cleavable SMCC linker.
    DM4-SMCC
  • HY-130812
    Gemcitabine-O-Si(di-iso)-O-Mc
    98.82%
    Gemcitabine-O-Si(di-iso)-O-Mc is a agent-linker conjugate for ADC with potent antitumor activity by using Gemcitabine (a pyrimidine nucleoside analog antimetabolite and an antineoplastic agent; HY-17026), linked via the ADC linker.
    Gemcitabine-O-Si(di-iso)-O-Mc
  • HY-169322
    APL-1081
    99.79%
    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-W190943
    Azido-PEG4-Val-Cit-PAB-MMAE
    99.43%
    Azido-PEG4-Val-Cit-PAB-MMAE is a agent-linker conjugate for ADC by using the anti-mitotic agent, monomethyl auristatin E (MMAE, a tubulin inhibitor), linked via the cleavable linker Azido-PEG4-Val-Cit-PAB-OH. Azido-PEG4-Val-Cit-PAB-MMAE 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.
    Azido-PEG4-Val-Cit-PAB-MMAE
  • HY-139726
    Mal-PEG4-Val-Cit-PAB-MMAE
    98.64%
    Mal-PEG4-Val-Cit-PAB-MMAE is part of a drug-linker conjugate for ADC. Mal-PEG4-Val-Cit-PAB-MMAE contains a degradable ADC linker Mal-PEG4-Val-Cit-PAB (HY-126672) and a potent tubulin inhibitor MMAE (HY-15162).
    Mal-PEG4-Val-Cit-PAB-MMAE
  • HY-160788
    DBCO-β-Glu-PEG12-Exatecan
    98.63%
    DBCO-β-Glu-PEG12-Exatecan (Compound 107) is an inhibitor for topoisomerase I. DBCO-β-Glu-PEG12-Exatecan can be used as a Drug-Linker Conjugate for ADC molecule.
    DBCO-β-Glu-PEG12-Exatecan
  • HY-101152
    SG3199-Val-Ala-PAB
    SG3199-Val-Ala-PAB is an intermediate of Tesirine synthesis. Tesirine is a agent-linker conjugate for ADC which can be used for the research of several cancers.
    SG3199-Val-Ala-PAB
  • HY-164788
    GGFG-PAB-MMAE
    99.33%
    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-19697
    Aminocaproyl-Val-Cit-PABC-MMAE
    99.89%
    Aminocaproyl-Val-Cit-PABC-MMAE is an Drug-linker conjugate for ADC.
    Aminocaproyl-Val-Cit-PABC-MMAE
  • HY-156758
    Mal-PEG8-Val-Cit-PAB-MMAF
    99.97%
    Mal-PEG8-Val-Cit-PAB-MMAF is a drug-linker conjugate for ADC. Mal-PEG8-Val-Cit-PAB-MMAF contains a cleavable ADC linker and a potent tubulin inhibitor MMAE (HY-15162).
    Mal-PEG8-Val-Cit-PAB-MMAF
  • HY-W190927
    MC-Val-Cit-Doxorubicin
    99.67%
    MC-Val-Cit-Doxorubicin (MC-Val-Cit-PAB-Doxorubicin) is drug-linker conjugate for ADC. The maleimide can conjugate with thiol containing molecules. Doxorubicin is an anthracycline antibiotic with antineoplastic activity
    MC-Val-Cit-Doxorubicin
  • HY-126686
    Mal-Phe-C4-VC-PAB-MMAE
    99.54%
    Mal-Phe-C4-VC-PAB-MMAE is made by MMAE conjugated to Mal-Phe-C4-VC-PAB linker. Monomethyl auristatin E (MMAE), a potent tubulin inhibitor, is a toxin payload in antibody agent conjugate.
    Mal-Phe-C4-VC-PAB-MMAE
  • HY-148127
    TAM558
    99.48%
    TAM558 is a payload molecule used for the synthesis of OMTX705. OMTX705 is a humanized anti-fibroblast-activating protein (FAP) antibody conjugated to the cytolysin TAM470 (HY-148128), with antitumor activity.
    TAM558
  • HY-160807
    DBM-GGFG-NH-O-CO-Exatecan
    DBM-GGFG-NH-O-CO-Exatecan (Example 4, Compound 14) is a conjugate of an ADC drug toxin molecule and a linker. DBM-GGFG-NH-O-CO-Exatecan is a complete antibody-drug conjugate intermediate that integrates a potent camptothecin-based toxin, a cleavable peptide linker (GGFG), and a reactive terminus that can directly conjugate to antibodies.
    DBM-GGFG-NH-O-CO-Exatecan
  • HY-176415
    Cys-MC-GGFG-Dxd
    99.01%
    Cys-MC-GGFG-Dxd is a cysteine-modified, cleavable ADC drug-linker conjugate. Cys-MC-GGFG-Dxd consists of a maleimidocaproyl-glycine-glycine-L-phenylalanine-glycine (MC-GGFG) linker and an Exatecan (HY-13631) derivative (DXd) (HY-13631D) payload. Cys-MC-GGFG-Dxd can be further conjugated to anti-HER2 IgG1κ antibody for the synthesis of antibody-drug conjugates (ADC), such as the breast cancer-targeting ADC compound Fam-trastuzumab deruxtecan-nxki (Enhertu).
    Cys-MC-GGFG-Dxd
  • HY-164995
    L1BC8
    99.20%
    L1BC8 (compound 13a) is a BRD4 PROTAC degrader with anticancer effects. L1BC8 is also a drug-linker conjugate for ADC that can be used for the synthesis of ADCs. The resulting BRD4-degrader antibody conjugates exhibit potent and antigen-dependent BRD4 degradation and antiproliferation activities in cell-based experiments. (Pink: BRD4 ligand (HY-129939); Blue: VHL ligand (HY-125845); Black: linker (HY-171663)).
    L1BC8
  • HY-177880
    2-MSP-5-HA-VC-PAB-MMAE
    98.59%
    2-MSP-5-HA-VC-PAB-MMAE (Compound B-1) is a Drug-Linker Conjugates for ADC. 2-MSP-5-HA-VC-PAB-MMAE consists of the ADC Cytotoxin Monomethyl auristatin E (HY-15162) and a linker 2-MSP-5-HA-VC-PAB-OH (HY-177905). 2-MSP-5-HA-VC-PAB-MMAE can be used for synthesis of ADCs.
    2-MSP-5-HA-VC-PAB-MMAE
  • HY-141536
    PSMA-ALB-56
    98.92%
    PSMA-ALB-56 is a PSMA-targeting radioligand designed by combining the glutamate-urea PSMA-binding entity and an albumin binder.
    PSMA-ALB-56

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