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-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-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
    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-153947
    PB089
    		99.98%
    PB089 is a Drug-liker containing a PEG unit and a cleavable linker attached to Exatecan.
    PB089
  • HY-136261
    DM1-PEG4-DBCO
    		98.04%
    DM1-(PEG)4-DBCO is a agent-linker conjugate composed of a potent microtubulin inhibitor DM1 and a linker DBCO-PEG4-Ahx to make antibody agent conjugate (ADC). Mertansine (DM1) is a microtubulin inhibitor and is an antibody-conjugatable maytansinoid that is developed to overcome systemic toxicity associated with maytansine and to enhance tumor-specific delivery. DM1-PEG4-DBCO is a click chemistry reagent, it contains a DBCO group that can undergo strain-promoted alkyne-azide cycloaddition (SPAAC) with molecules containing Azide groups.
    DM1-PEG4-DBCO
  • HY-147307
    MC-Gly-Gly-Phe-Gly-Cyclobutanecarboxylic-Exatecan
    		99.55%
    MC-Gly-Gly-Phe-Gly-Cyclobutanecarboxylic-Exatecan is a agent-linker conjugate for ADC, contains the ADC linker (MC-Gly-Gly-Phe-Gly-Cyclobutanecarboxylic acid) and a DNA topoisomerase I inhibitor Exatecan (HY-13631). MC-Gly-Gly-Phe-Gly-Cyclobutanecarboxylic-Exatecan synthesized ADC can be used in study of cancer.
    MC-Gly-Gly-Phe-Gly-Cyclobutanecarboxylic-Exatecan
  • 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-160157
    IM-2
    IM-2 is an ADC linker used in the synthesis of antibody-drug conjugates (ADCs).
    IM-2
  • HY-169322
    APL-1081
    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-156758
    Mal-PEG8-Val-Cit-PAB-MMAF
    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-101982A
    (Rac)-Lys-SMCC-DM1
    		98.18%
    (Rac)-Lys-SMCC-DM1 ((Rac)-Lys-Nε-MCC-DM1) is the racemate of Lys-SMCC-DM1 (HY-101982). Lys-SMCC-DM1 is a linker-payload component that has the potential to inhibit tubulin polymerization. Lys-SMCC-DM1 is the active metabolite of T-DM1.
    (Rac)-Lys-SMCC-DM1
  • HY-15740
    Mc-MMAD
    		98.39%
    Mc-MMAD is a protective group (maleimidocaproyl)-conjugated MMAD. MMAD is a potent tubulin inhibitor. Mc-MMAD is a agent-linker conjugate for ADC.
    Mc-MMAD
  • HY-128899
    MC-Val-Cit-PAB-Auristatin E
    MC-Val-Cit-PAB-Auristatin E is a agent-linker conjugate for ADC with potent antitumor activity by using Auristatin E (a cytotoxic tubulin modifier), linked via the ADC linker MC-Val-Cit-PAB.
    MC-Val-Cit-PAB-Auristatin E
  • HY-128897
    MC-VC-PABC-DNA31
    		98.71%
    MC-VC-PABC-DNA31 is a agent-linker conjugate for ADC with potent antitumor activity by using DNA31 (a potent RNA polymerase inhibitor), linked via the ADC linker MC-VC-PABC.
    MC-VC-PABC-DNA31
  • HY-126532
    Fmoc-Val-Cit-PAB-Duocarmycin TM
    		99.44%
    Fmoc-Val-Cit-PAB-Duocarmycin TM is a agent-linker conjugate for ADC by using the antitumor antibiotic, Duocarmycin TM, linked via Fmoc-Val-Cit-PAB.
    Fmoc-Val-Cit-PAB-Duocarmycin TM
  • 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-132158
    MC-AAA-NHCH2OCH2COO-7-aminomethyl-10-methyl-11-fluoro camptothecin
    MC-AAA-NHCH2OCH2COO-7-aminomethyl-10-methyl-11-fluoro camptothecin (compound 21a), a camptothecin payload, can be conjugated to a monoclonal antibody (mAb) for the synthesis of camptothecin antibody-drug conjugate (ADC).
    MC-AAA-NHCH2OCH2COO-7-aminomethyl-10-methyl-11-fluoro camptothecin
  • HY-153739
    N3-PEG3-VC-PAB-MMAF
    		99.95%
    N3-PEG3-VC-PAB-MMAF (Comp T-88-5) is a drug-linker conjugate containing the ADC linker N3-PEG3-VC-PAB and the tubulin inhibitor MMAF. N3-PEG3-VC-PAB-MMAF 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.
    N3-PEG3-VC-PAB-MMAF
Drug-Linker Conjugates for ADC Isoform Comparison

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