1. シグナル伝達
  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.

製品番号 製品名 製品効果 純度 構造式
  • HY-163549
    APN-PEG5-VC-PAB-MMAE
    APN-PEG5-VC-PAB-MMAE is a drug-linker conjugate part of INA03 (a transferrin-competitive antibody-drug conjugate against CD71).
    APN-PEG5-VC-PAB-MMAE
  • 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-164837
    VcMMAE-Eribulin 98.87%
    VcMMAE-Eribulin is a Drug-Linker Conjugates for ADC, which is composed of a linker and a toxic molecule MMAE (HY-15162) (Microtubule inhibitor) and Eribulin (HY-13442) (Microtubule inhibitor). VcMMAE-Eribulin can be used for ADC synthesis.
    VcMMAE-Eribulin
  • 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-128909
    MC-Val-Cit-PAB-rifabutin
    MC-Val-Cit-PAB-rifabutin is a agent-linker conjugate for ADC with potent antitumor activity by using rifabutin (an DNA-dependent RNA polymerase inhibitor), linked via the ADC linker MC-Val-Cit-PAB.
    MC-Val-Cit-PAB-rifabutin
  • HY-128906
    MC-Val-Cit-PAB-Retapamulin 99.37%
    MC-Val-Cit-PAB-Retapamulin is a agent-linker conjugate for ADC with potent antitumor activity by using Retapamulin (a ribosome inhibitor), linked via the ADC linker MC-Val-Cit-PAB.
    MC-Val-Cit-PAB-Retapamulin
  • 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-177879
    2-MSP-5-HA-VA-PAB-Exatecan
    2-MSP-5-HA-Val-Cit-PAB-Exatecan (A-24) is a drug-linker conjugate for ADC. 2-MSP-5-HA-Val-Cit-PAB-Exatecan consists of Exatecan (HY-13631) and a linker. 2-MSP-5-HA-Val-Cit-PAB-Exatecan can be used for synthesis of ADCs.
    2-MSP-5-HA-VA-PAB-Exatecan
  • HY-131088
    N3-PEG8-Phe-Lys-PABC-Gefitinib
    N3-PEG8-Phe-Lys-PABC-Gefitinib is a agent-linker conjugate for ADC with potent antitumor activity by using the anti-tumor agent, Gefitinib (HY-50895) (orally active EGFR tyrosine kinase inhibitor), linked via the cleavable linker N3-PEG8-Phe-Lys-PABC. N3-PEG8-Phe-Lys-PABC-Gefitinib 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-PEG8-Phe-Lys-PABC-Gefitinib
  • HY-131088A
    N3-PEG8-Phe-Lys-PABC-Gefitinib TFA
    N3-PEG8-Phe-Lys-PABC-Gefitinib TFA is a agent-linker conjugate for ADC with potent antitumor activity by using the anti-tumor agent, Gefitinib (HY-50895) (orally active EGFR tyrosine kinase inhibitor), linked via the cleavable linker N3-PEG8-Phe-Lys-PABC. N3-PEG8-Phe-Lys-PABC-Gefitinib TFA 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-PEG8-Phe-Lys-PABC-Gefitinib TFA
  • HY-148346A
    STING agonist-20-Ala-amide-PEG2-C2-NH2 TFA 98.30%
    STING agonist-20-Ala-amide-PEG2-C2-NH2 (Compound 30b) TFA is an active scaffold comprising a stimulator of interferon genes (STING). STING agonist-20-Ala-amide-PEG2-C2-NH2 TFA can be used to synthesize immune-stimulating antibody conjugate (ISAC). STING agonist-20-Ala-amide-PEG2-C2-NH2 TFA can be used for the research of cancer.
    STING agonist-20-Ala-amide-PEG2-C2-NH2 TFA
  • HY-145989S
    Aminobenzenesulfonic auristatin E-d8 98.02%
    Aminobenzenesulfonic auristatin E-d8 is the deuterium labeled Aminobenzenesulfonic auristatin E. Aminobenzenesulfonic auristatin E is a drug-linker conjugate for ADC. Aminobenzenesulfonic auristatin E has potent antitumor activity by using Auristatin E (a cytotoxic tubulin modifier), linked via the ADC linker Aminobenzenesulfonic.
    Aminobenzenesulfonic auristatin E-d<sub>8</sub>
  • HY-186191
    LY-22CD
    LY-22CD is a Drug-Linker Conjugates for ADC. LY-22CD consists of an ADC payload and a linker, and can be used for ADC synthesis.
    LY-22CD
  • HY-152916
    mp-dLAE-PABC-MMAE 98.31%
    mp-dLAE-PABC-MMAE is a agent-linker conjugate for ADC. mp-dLAE-PABC-MMAE contains a potent tubulin inhibitor Monomethyl auristatin E (HY-15162). mp-dLAE-PABC-MMAE can be used to synthesis antibody-drug conjugates (ADCs).
    mp-dLAE-PABC-MMAE
  • 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-147286A
    Ac-Lys-Val-Cit-PABC-MMAE formic 99.96%
    Ac-Lys-Val-Cit-PABC-MMAE (formic) 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 inhibitorMonomethyl auristatin E (HY-15162).
    Ac-Lys-Val-Cit-PABC-MMAE formic
  • HY-185664
    2-MSP-2-(pent-4-yn-1-yloxy)acetic acid-VC-PAB-Eribulin
    2-MSP-2-(pent-4-yn-1-yloxy)acetic acid-VC-PAB-Eribulin is a drug-linker conjugate comprising Eribulin (HY-13442), can be used for preparation of multi-projectile antibody-drug conjugates (ADCs).2-MSP-2-(pent-4-yn-1-yloxy)acetic acid-VC-PAB-Eribulin can be used for the research of tumor diseases.
    2-MSP-2-(pent-4-yn-1-yloxy)acetic acid-VC-PAB-Eribulin
  • HY-168317
    LNK2-S
    LNK2-S is a conjugated compound of toxin molecule Exatecan (HY-13631) and Linker, which can be used to synthesize ADC molecule.
    LNK2-S
  • HY-156897
    Val-Cit-amide-Ph-Maytansine 98.01%
    Val-Cit-amide-Ph-Maytansine is an antibody and bispecific antigen-binding mol. that bind hepatocyte growth factor receptor c-Met (MET) or antibody-drug conjugates (ADCs).
    Val-Cit-amide-Ph-Maytansine

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