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

Drug-Linker Conjugates for ADC

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-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-153947
    PB089
    		99.98%
    PB089 is a Drug-liker containing a PEG unit and a cleavable linker attached to Exatecan.
    PB089
  • 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-126683
    Mal-C6-α-Amanitin
    		98.48%
    Mal-C6-α-Amanitin is a agent-linker conjugate for ADC with potent antitumor activity by using α-Amanitin (an RNA polymerase II inhibitor), linked via the ADC linker Mal-C6.
    Mal-C6-α-Amanitin
  • HY-112616
    NAMPT inhibitor-linker 2
    		98.11%
    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-147281
    BAY 1135626
    		99.19%
    BAY 1135626 is used to synthesize BAY 1129980, and use to anti-tumor research. BAY 1129980 is a Auristatin-based anti-C4.4A (LYPD3) antibody–agent conjugate (ADC), is used to non–small cell lung cancer (NSCLC) research.
    BAY 1135626
  • HY-160015
    CB07-Exatecan
    		98.97%
    CB07-Exatecan is an ADC drug-Linker conjugate that can be used for the synthesis of ADCs. ADC conjugated with CB07-Exatecan and trastuzumab inhibits the growth of HER2-positive cancer cells. CB07-Exatecan can be used in cancer research.
    CB07-Exatecan
  • HY-147204
    Mc-Alanyl-Alanyl-Asparagine-PAB-MMAE
    		98.26%
    Mc-Alanyl-Alanyl-Asparagine-PAB-MMAE (compound S6) is a potent anticancer agent, which can be specific activated by tumor microenvironment. Mc-Alanyl-Alanyl-Asparagine-PAB-MMAE can suppress tumor growth in mice (extracted from patent CN104147612A).
    Mc-Alanyl-Alanyl-Asparagine-PAB-MMAE
  • HY-152121
    Glucocorticoid receptor agonist-1 phosphate Ala-Ala-Mal
    Glucocorticoid receptor agonist-1 phosphate Ala-Ala-Mal is a glucocorticoid receptor agonist. Glucocorticoid receptor agonist-1 phosphate Ala-Ala-Mal can be used in anti-CD40 antibody agent conjugate (ADC). Glucocorticoid receptor agonist-1 phosphate Ala-Ala-Mal can be used for the research of inflammation and immune regulation.
    Glucocorticoid receptor agonist-1 phosphate Ala-Ala-Mal
  • HY-156377
    Biotin-PEG7-Maleimide
    		98.60%
    Biotin-PEG7-Maleimide is a biotinylation reagent that reacts with thiol groups (SH). Biotin-PEG7-Maleimide can be used as Drug-Linker Conjugates for ADCs.
    Biotin-PEG7-Maleimide
  • HY-112615
    NAMPT inhibitor-linker 1
    		98.08%
    NAMPT inhibitor-linker 1 is a agent-linker conjugates for ADC, composed of an NAMPT inhibitor as a payload, and a linker. ADC-3 consists of an NAMPT inhibitor-linker 1 and an anti-c-Kit monoclonal antibody, exihibits potent activity against c-Kit expressing cell lines such as GIST-T1 and NCI-H526 cells, with IC50s of <3 pM and 9 pM, respectively.
    NAMPT inhibitor-linker 1
  • 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-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-160157
    IM-2
    IM-2 is an ADC linker used in the synthesis of antibody-drug conjugates (ADCs).
    IM-2
  • HY-131451
    Mc-Phe-Lys-PAB-MMAE
    Mc-Phe-Lys-PAB-MMAE (Compound 2) is a drug-linker conjugate for ADC, and can be used for synthesis of ADCs.
    Mc-Phe-Lys-PAB-MMAE
  • HY-148871
    Mc-Val-Cit-PAB-Gefitinib chloride
    		98.69%
    Mc-Val-Cit-PAB-Gefitinib chloride is a agent-linker conjugates for ADC. Mc-Val-Cit-PAB-Gefitinib chloride consists of Gefitinib (HY-50895) (an EGFR tyrosine kinase inhibitor) and the ADC linker Mc-Val-Cit-PAB.
    Mc-Val-Cit-PAB-Gefitinib chloride
  • 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-157284
    Cys-mc-MMAE
    		99.85%
    Cys-mc-MMAE is a Drug-Linker Conjugates for ADC, and consists of Monomethyl auristatin E (HY-15162) and a linker. Cys-mc-MMAE can be used for synthesis of ADCs.
    Cys-mc-MMAE
  • HY-156691A
    TLR7/8 agonist 4 hydroxy-PEG6-acid hydrochloride
    TLR7/8 agonist 4 hydroxy-PEG6-acid hydrochloride is a Drug-Linker Conjugates for ADC. TLR7/8 agonist 4 hydroxy-PEG6-acid hydrochloride is the hydrochloride form of TLR7/8 agonist 4 hydroxy-PEG6-acid. TLR7/8 agonist 4 hydroxy-PEG6-acid consists of TLR7/8 agonist 4 (HY-139017) and a linker Hydroxy-PEG6-acid (HY-133050), and can be used for synthesis of ADCs.
    TLR7/8 agonist 4 hydroxy-PEG6-acid hydrochloride
  • 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
Drug-Linker Conjugates for ADC Isoform Comparison

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