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-128951
    AMCC-DM1
    AMCC-DM1 is a drug-linker conjugate composed of a potent a tubulin inhibitor DM4 and a linker AMCC to make antibody drug conjugate. AMCC is a noncleavable linker.
    AMCC-DM1
  • HY-179276
    TAK-500 drug-linker
    TAK-500 drug-linker is a drug-linker complex consisting of the STING protein agonist Dazostinag (HY-152861) and a linker (HY-179279). TAK-500 drug-linker can be used to synthesize ADCs.
    TAK-500 drug-linker
  • HY-169323
    APL-1091
    APL-1091 (Mal-Exo-EEVC-MMAE) is part of a Drug-linker conjugate for ADC. APL-1091 contains a Mal-Exo-EEVC (HY-169353) linker and MMAE (HY-15162) (Microtubule inhibitor). APL-1091 can be used for ADC synthesis.
    APL-1091
  • HY-155313
    β-Glucuronide-NB-bis[N(Me)-methyl ester]-MMAE
    β-Glucuronide-NB-bis[N(Me)-methyl ester]-MMAE (compound 20) is auristatins-glucuronide conjugate. Antitumor agent-122 shows in vitro antiproliferative activities against β-glucuronidase pretreated and untreated cancer cells with an IC50 value of 5.7 nM - 9.7 nM. Antitumor agent-122 shows potent antitumor efficacy in HCT-116 xenograft mouse model without inducing side effects.
    β-Glucuronide-NB-bis[N(Me)-methyl ester]-MMAE
  • HY-158137
    Val-Cit-PAB-DEA-Dxd
    Val-Cit-PAB-DEA-Dxd (compound 81) is a Drug-Linker Conjugates for ADC, which is composed of a linker and a toxic molecule Dxd (DNA topoisomerase I inhibitor). Val-Cit-PAB-DEA-Dxd can be used for ADC synthesis.
    Val-Cit-PAB-DEA-Dxd
  • HY-177413
    Tub114
    Tub114 is a drug-linker conjugate for ADC. Tub114 is a Tubulysin B (HY-N1243) analog with a stable hydrophilic linker. Tub114 can be used for synthesis of ADCs.
    Tub114
  • HY-185101
    MC-AcLys-GDEVD-PABC-Exatecan
    MC-AcLys-GDEVD-PABC-Exatecan (MC-AcLys-GDEVD-PABC-DX8951) is a agent-linker conjugate for ADC. MC-AcLys-GDEVD-PABC-Exatecan is a DX8951 (a DNA topoisomerase I inhibitor) derivative with a novel caspase-3 cleavable peptide linker MC-AcLys-GDEVD-PABC linker. MC-AcLys-GDEVD-PABC-Exatecan can be used to prepare DX8951 antibody conjugate (ADC), and it exhibites significant bystander effect mediated by the caspase-3-triggered extracellular cleavage of the linker, enhancing payload release into the tumor microenvironment.
    MC-AcLys-GDEVD-PABC-Exatecan
  • HY-157501
    PC6-VC-PAB-MMAE
    PC6-VC-PAB-MMAE is a Drug-Linker Conjugates for ADC. PC6-VC-PAB-MMAE consists of the ADC Cytotoxin MMAE (HY-15162) and a linker. PC6-VC-PAB-MMAE can be used for synthesis of ADCs.
    PC6-VC-PAB-MMAE
  • HY-160087
    SG3376
    SG3376 is an antibody-drug conjugate (ADC) targeting human epidermal growth factor receptor 2 (HER2). SG3376 is promising for research of HER2-overexpressing cancers (e.g., breast, gastric cancer).
    SG3376
  • HY-164707
    MC7
    MC7 is a drug-linker conjugate for ADC and can be used for ADC synthesis. The payload is a NAMPT inhibitor (HY-402237).
    MC7
  • HY-139325
    NHS-Modified MMAF
    NHS-Modified MMAF (WO2012143499A2, intermediat 210) is an intermediate which can be used for producing the anti-mesothelin binder-agent conjugates (ADCs).
    NHS-Modified MMAF
  • HY-178260
    LM-D01
    LM-D01 is a Drug-Linker Conjugates for ADC. LM-D01 consists of the ADC Cytotoxin Exatecan-3-amine (HY-178265) and a linker MC-GGFG-NH-CH2-O-propionic acid (HY-178266). LM-D01 can be used for synthesis of ADCs.
    LM-D01
  • HY-141662
    2',3'-cGAMP-C2-PPA
    2’,3’-cGAMP-C2-PPA is a cyclic dinucleotide interferon gene-stimulating protein (STING) agonist. 2’,3’-cGAMP-C2-PPA is a drug conjugated conjugate used to target antibody-drug conjugated conjugate (ADC) for the treatment of cancer. 2’,3’-cGAMP-C2-PPA can be used in the study of immune and tumor-related diseases.
    2',3'-cGAMP-C2-PPA
  • HY-136321
    MC-betaglucuronide-MMAE-2
    MC-betaglucuronide-MMAE-2 is a agent-linker conjugate for ADC with potent antitumor activity by using MMAE (a tubulin polymerization inhibitor), linked via the cleavable ADC linker MC-betaglucuronide.
    MC-betaglucuronide-MMAE-2
  • HY-176766
    Mal-PEG8-Val-Ala-Exatecan
    		99.55%
    Mal-PEG8-Val-Ala-Exatecan (Compound 1033) is a Drug-Linker Conjugates for ADC, which is composed of Exatecan (HY-13631) and a linker. Mal-PEG8-Val-Ala-Exatecan can be used for ADC synthesis.
    Mal-PEG8-Val-Ala-Exatecan
  • HY-139957
    Mal-amido-PEG8-Val-Ala-PAB-SG3200
    Mal-amido-PEG8-Val-Ala-PAB-SG3200 is a conjugate for antibody-drug conjugate (ADC) (extracted from patent WO2016166300A1).
    Mal-amido-PEG8-Val-Ala-PAB-SG3200
  • HY-141148
    7-O-(Cbz-N-amido-PEG4)-paclitaxel
    7-O-(Cbz-N-amido-PEG4)-paclitaxel is a PEG-class Drug-linker conjugates for ADC, containing a paclitaxel moiety and a amino group. The amine group is reactive with carboxylic acids, activated NHS esters, carbonyls (ketone, aldehyde) etc. 7-O-(Cbz-N-amido-PEG4)-paclitaxel can be used in the synthesis of Antibody-Drug Conjugates (ADCs).
    7-O-(Cbz-N-amido-PEG4)-paclitaxel
  • HY-168285
    LE01
    LE01 is a drug-linker conjugate for ADC. LE01 contains a ADC linker and a DNA topoisomerase I inhibitor DXd (HY-13631D). LE01 can be used to synthesize HER2-targeting ADC (HER2-LE01).
    LE01
  • HY-144630
    diSPhMC-Asn-Pro-Val-PABC-MMAE
    diSPhMC-Asn-Pro-Val-PABC-MMAE (compound 9) is a potent ADC Linker used in the synthesis of antibody-drug conjugates (ADCs).
    diSPhMC-Asn-Pro-Val-PABC-MMAE
  • HY-164829
    Mal-C5-Gly-Gly-Phe-MMAE
    Mal-C5-Gly-Gly-Phe-MMAE (Compound S5) is a drug-linker conjugate for ADC. Mal-C5-Gly-Gly-Phe-MMAE consists of MMAE (HY-15162) and a linker. Mal-C5-Gly-Gly-Phe-MMAE can be used for synthesis of ADCs and for cancer research.
    Mal-C5-Gly-Gly-Phe-MMAE
Drug-Linker Conjugates for ADC Isoform Comparison

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