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-128943
    MAC glucuronide phenol-linked SN-38
    		98.49%
    MAC glucuronide phenol-linked SN-38 is a pH-susceptible lactone MAC glucuronide phenol-linked SN-38 (DNA topoisomerase I inhibitor) agent linker. MAC glucuronide phenol-linked SN-38 is cytotoxic across L540cy cells and Ramos cells with IC50 values of 113 and 67 ng/mL, respectively.Albumin-coupled MAC glucosidol-linked SN-38 shows good stability in mouse plasma.
    MAC glucuronide phenol-linked SN-38
  • HY-153345
    Glucocorticoid receptor agonist-1 phosphate(2,6-difluoro) Ala-Ala-Br
    		99.67%
    Glucocorticoid receptor agonist-1 phosphate(2,6-difluoro) Ala-Ala-Br is an Drug-linker conjugates for ADC that can be used as a reaction reagent for the synthesis of anti-CD40 antibody agent conjugates (ADCs).
    Glucocorticoid receptor agonist-1 phosphate(2,6-difluoro) Ala-Ala-Br
  • HY-136287
    DBM-MMAF
    		99.65%
    DBM-MMAF is a agent-linker conjugate composed of a potent antitubulin agent MMAF and a linker DBM to make antibody agent conjugate (ADC).
    DBM-MMAF
  • HY-164088
    DBM-C5-VC-PAB-MMAE
    		99.45%
    DBM-C5-VC-PAB-MMAE (Compound 3a) is a Drug-Linker conjugate for ADC. DBM-C5-VC-PAB-MMAE is composed of a linker C5-VC-PAB with a maleimide group DBM and an ADC toxin MMAE (HY-15162).
    DBM-C5-VC-PAB-MMAE
  • HY-157544
    PC5-VC-PAB-MMAE
    		99.76%
    PC5-VC-PAB-MMAE consists the ADCs linker (PC5-VC-PAB) and potent tubulin inhibitor (MMAE). PC5-VC-PAB-MMAE is a agent-linker conjugate for ADC.
    PC5-VC-PAB-MMAE
  • 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-100567
    MAL-di-EG-Val-Cit-PAB-MMAE
    MAL-di-EG-Val-Cit-PAB-MMAE consists the ADCs linker (MAL-di-EG-Val-Cit-PAB) and potent tubulin inhibitor (MMAE).
    MAL-di-EG-Val-Cit-PAB-MMAE
  • HY-157465
    MA-PEG4-VC-PAB-DMEA-duocarmycin DM
    		99.84%
    MA-PEG4-VC-PAB-DMEA-duocarmycin DM is a drug-linker conjugate for ADC by using the DNA minor-groove alkylator Duocarmycin DM (HY-130978), linked via MA-PEG4-vc-PAB-DMEA (HY-126668).
    MA-PEG4-VC-PAB-DMEA-duocarmycin DM
  • HY-153031
    Val-Cit-PAB-Exatecan
    		99.79%
    Val-Cit-PAB-Exatecan (Val-Cit-PAB-DX8951) is a agent-linker conjugate for ADC. Val-Cit-PAB-Exatecan is composed of a DNA topoisomerase I DX-8951 (HY-13631) and a cathepsin cleavable ADC linker.
    Val-Cit-PAB-Exatecan
  • HY-147286
    Ac-Lys-Val-Cit-PABC-MMAE
    		99.94%
    Ac-Lys-Val-Cit-PABC-MMAE is a agent-linker conjugate for ADC. Ac-Lys-Val-Cit-PABC-MMAE contains the ADC linker (peptide Ac-Lys-Val-Cit-PABC) and a potent tubulin polymerization inhibitor MMAE (HY-15162).
    Ac-Lys-Val-Cit-PABC-MMAE
  • HY-164367
    Mal-Bal-Ph(β-D-Glucose)-7-MAD-MDCPT
    		98.19%
    DBCO-PEG2-C2-acid is an ADC Linker. DBCO-PEG2-C2-acid can be used to synthesize Antibody-Drug Conjugates (ADCs).
    Mal-Bal-Ph(β-D-Glucose)-7-MAD-MDCPT
  • HY-153263
    (Aminooxy)acetamide-Val-Cit-PAB-MMAE
    (Aminooxy)acetamide-Val-Cit-PAB-MMAE (MMAE 5) is an intermediate used in the synthetic preparation of drug-linker conjugates for ADC. (Aminooxy)acetamide-Val-Cit-PAB-MMAE is conjugated to polyamide via oxime bond formation to form MMAE polyamide conjugate. Then MMAE polyamide conjugate can be conjugated to Trastuzumab, to make ADC.
    (Aminooxy)acetamide-Val-Cit-PAB-MMAE
  • HY-137883
    Glucocorticoid receptor agonist-1 phosphate Gly-Glu-Br
    		99.62%
    Glucocorticoid receptor agonist-1 phosphate Gly-Glu-Br is a drug-linker conjugate for ADC that can be used to synthesize ABBV-154, ABBV-927, ABBV-368 or their analogs.
    Glucocorticoid receptor agonist-1 phosphate Gly-Glu-Br
  • HY-148436
    Glucocorticoid receptor agonist-2 Ala-Ala-Mal
    Glucocorticoid receptor agonist-2 Ala-Ala-Mal (compound 79) can be used to synthesize anti-inflammatory ADC molecules. Glucocorticoid receptor agonist-2 is an active reference for ABBV-3373.
    Glucocorticoid receptor agonist-2 Ala-Ala-Mal
  • HY-112616
    NAMPT inhibitor-linker 2
    		99.35%
    NAMPT inhibitor-linker 2 is a agent-linker conjugates for ADC, composed of an NAMPT inhibitor as a payload, and a linker. ADC-4 consists of an NAMPT inhibitor-linker 2 and an anti-c-Kit monoclonal antibody, exihibits potent activity against c-Kit expressing cell lines such as GIST-T1 and NCI-H526, with IC50s of <7 pM and 40 pM, respectively.
    NAMPT inhibitor-linker 2
  • HY-137882
    Glucocorticoid receptor agonist-1 Ala-Ala-Mal
    		99.94%
    Glucocorticoid receptor agonist-1 Ala-Ala-Mal (compound 88) is a glucocorticosteroid, and an agonist of glucocorticoid receptor. Glucocorticoid receptor agonist-1 Ala-Ala-Mal can be conjugated with Adalimumab (HY-P9908) to prepare an ADC.
    Glucocorticoid receptor agonist-1 Ala-Ala-Mal
  • 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-159072
    Mal-Val-Ala-PAB-N(SO2Me)-Exatecan
    		99.11%
    Mal-Val-Ala-PAB-N(SO2Me)-Exatecan (Compound LE14) is a conjugate of an ADC toxin Exatecan (HY-13631) and a linker Mal-Val-Ala-PAB-N(SO2Me). Mal-Val-Ala-PAB-N(SO2Me)-Exatecan can be used for synthesis of ADC FZ-AD005. FZ-AD005 is a delta-like ligand 3 (DLL3, KD=58.3 pM) targeting ADC, that exhibits antitumor efficacy against SCLC cancer.
    Mal-Val-Ala-PAB-N(SO2Me)-Exatecan
  • HY-163099
    P5(PEG24)-VC-PAB-Exatecan
    		99.74%
    P5(PEG24)-VC-PAB-Exatecan (LP5) is a drug-linker conjugate composed of a potent a DNA Topoisomerase I inhibitor Exatecan (HY-13631) and a linker P5(PEG24)-VC-PAB to make antibody agent conjugate (ADC). P5(PEG24)-VC-PAB-Exatecan can be used for the research of tumor.
    P5(PEG24)-VC-PAB-Exatecan
  • 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
Drug-Linker Conjugates for ADC Isoform Comparison

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