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-139909
    CL2E-SN38
    CL2E-SN-38, a highly releasable and structurally stable antibody-SN-38-conjugate, is a part of the antibody drug conjugate (ADC). SN-38, the active metabolite of Irinotecan from camptothecins, is an Topoisomerase I inhibitor.
    CL2E-SN38
  • HY-160247
    Boc-Lys-PEG8-N-bis(D-glucose)
    Boc-Lys-PEG8-N-bis(D-glucose) (compound 89-5) is a drug linker that can be used in the synthesis of antibody-drug conjugates (ADCs) extracted from patent WO2023280227A2.
    Boc-Lys-PEG8-N-bis(D-glucose)
  • HY-128910
    MC-VC(S)-PABQ-Tubulysin M
    MC-VC(S)-PABQ-Tubulysin M is a synthetic ADC drug-linker conjugate composed of the tubulin polymerization inhibitor Tubulysin M (an ADC Cytotoxin) (HY-N7053) and MC-VC(S)- PABQ (an ADC linker) is connected. MC-VC(S)-PABQ-Tubulysin M is effective against multidrug-resistant lymphoma cell lines and tumors.
    MC-VC(S)-PABQ-Tubulysin M
  • HY-160143
    G3-VC-PAB-DMEA-Duocarmycin DM
    G3-VC-PAB-DMEA-Duocarmycin DM (Compound LD-1) is a duocarmycin-based linker molecule that can be used for ADC preparation..
    G3-VC-PAB-DMEA-Duocarmycin DM
  • HY-164836
    Deruxtecan-Eribulin
    Deruxtecan-Eribulin is a Drug-Linker Conjugates for ADC, which is composed of a linker and a toxic molecule Exatecan (HY-13631) (DNA topoisomerase I inhibitor) and Eribulin (HY-13442) (Microtubule inhibitor). Deruxtecan-Eribulin can be used for ADC synthesis.
    Deruxtecan-Eribulin
  • HY-171509
    Mal-N(Me)-C6-N(Me)-PNU-159682
    Mal-N(Me)-C6-N(Me)-PNU-159682 (Compound 27), an agent-linker conjugate for ADC, consists the ADC linker Mal-N(Me)-C6-N(Me) and a potent ADC cytotoxin PNU-159682. Mal-N(Me)-C6-N(Me)-PNU-159682 (Compound 27) selectively delivers the payload to CD46-expressing cells, where the linker is cleaved by cathepsin B to release PNU-159682, inducing DNA damage and apoptosis. Mal-N(Me)-C6-N(Me)-PNU-159682 shows durable tumor regression in xenograft (PDX) models of non-small cell lung cancer (NSCLC) and colorectal cancer (CRC).
    Mal-N(Me)-C6-N(Me)-PNU-159682
  • HY-153976
    Fmoc-Gly3-VC-PAB-MMAE
    Fmoc-Gly3-VC-PAB-MMAE is a Drug-Linker Conjugates for ADC. Fmoc-Gly3-VC-PAB-MMAE consists of Monomethyl auristatin E (HY-15162) and a linker.
    Fmoc-Gly3-VC-PAB-MMAE
  • HY-13631EG
    Deruxtecan (GMP)
    Deruxtecan (GMP) (MC-GGFG-DXD (GMP)) is Deruxtecan (HY-13631E) in GMP grade. GMP-grade small molecules can be used as auxiliary reagents in cell therapy. Deruxtecan is an ADC drug-linker conjugate composed of an DX-8951 derivative (DXd) and a maleimide-GGFG peptide linker, used for synthesizing Trastuzumab deruxtecan (HY-138298A) and Patritumab deruxtecan (HY-P99813).
    Deruxtecan (GMP)
  • HY-158351
    Mal-Val-Ala-PAB-NMe-CH2CH2-O-CO-Dazostinag
    Mal-Val-Ala-PAB-NMe-CH2CH2-O-CO-Dazostinag is a drug-linker conjugate for ADC.
    Mal-Val-Ala-PAB-NMe-CH2CH2-O-CO-Dazostinag
  • HY-141593
    Modified MMAF-C5-COOH
    Modified MMAF-C5-COOH is a agent-linker conjugate for ADC.
    Modified MMAF-C5-COOH
  • HY-153067
    Mal-cyclohexane-Gly-Gly-Phe-Gly-Exatecan
    Mal-cyclohexane-Gly-Gly-Phe-Gly-Exatecan is a coupling compound that can be used for the synthesis of ADC. Mal-cyclohexane-Gly-Gly-Phe-Gly-Exatecan synthesized ADC shows good antitumor activity in vitro and in vivo.
    Mal-cyclohexane-Gly-Gly-Phe-Gly-Exatecan
  • HY-160683
    MC-Gly-Gly-Phe-Gly-NH-CH2-O-amide-Eribulin
    MC-Gly-Gly-Phe-Gly-NH-CH2-O-amide-Eribulin (Compound 7) can be used as a linker-drug intermediate for the synthesis of antibody-drug conjugates (ADCs).
    MC-Gly-Gly-Phe-Gly-NH-CH2-O-amide-Eribulin
  • HY-125858B
    (S,R,S)-MI-1061
    (S,R,S)-MI-1061 is the isomer of MI-1061(HY-125858). (S,R,S)-MI-1061 can used to synthesize Antibody-Drug Conjugates (ADCs). MI-1061 is a potent, orally bioavailable, and chemically stable MDM2 (MDM2-p53 interaction) inhibitor (IC50=4.4 nM; Ki=0.16 nM). MI-1061 potently activates p53 and induces apoptosis in the SJSA-1 xenograft tumor tissue in mice. Anti-tumor activity.
    (S,R,S)-MI-1061
  • HY-173079
    TLR7 agonist 30
    TLR7 agonist 30 (compound 2) is an agent-linker conjugate for ADC. TLR7 agonist 30 contains a TLR7 agonist (compound 1) and a cleavable linker, and has potent anti-tumor activity.
    TLR7 agonist 30
  • HY-156896
    Val-Cit-amide-Cbz-N(Me)-Maytansine
    Val-Cit-amide-Cbz-N(Me)-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-Cbz-N(Me)-Maytansine
  • HY-160702
    DMBA-SIL-Mal-MMAE
    DMBA-SIL-Mal-MMAE is a cytotoxin-linker conjugate for ADC with potent antitumor activity by using the anti-mitotic agent, monomethyl auristatin E (MMAE, a tubulin inhibitor), linked DMBA-SIL-Mal.
    DMBA-SIL-Mal-MMAE
  • HY-128941
    CCK2R Ligand-Linker Conjugates 1
    CCK2R Ligand-Linker Conjugates 1 is a ligand-linker conjugate, which conjugates to the cytotoxic antimicrotubule agents Desacetyl Vinblastine Hydrazide (DAVBH) and Tubulysin B Hydrazide (TubBH) via a hydrophilic peptide linker.
    CCK2R Ligand-Linker Conjugates 1
  • HY-126493
    DM4-SPDP
    DM4-SPDP is a agent-linker conjugate composed of a potent antitubulin agent DM4 and a linker SMCC to make antibody agent conjugate. SPDP is a short-chain crosslinker for amine-to-sulfhydryl conjugation via NHS-ester and pyridyldithiol reactive groups that form cleavable (reducible) disulfide bonds with cysteine sulfhydryls.
    DM4-SPDP
  • HY-176202
    TLR7/8 agonist 12-PAB-(PEG4-Me)-Cit-Val-PEG2-amide-C2-MC
    TLR7/8 agonist 12-PAB-(PEG4-Me)-Cit-Val-PEG2-amide-C2-MC (compound LIV1-IMC (12) linker-payload) is a linker-payload conjugate, used in the synthesis of antibody-drug conjugates (ADCs).TLR7/8 agonist 12-PAB-(PEG4-Me)-Cit-Val-PEG2-amide-C2-MC contains TLR7/8 agonist (HY-170770) (ADC payload) and a linker (HY-176478).
    TLR7/8 agonist 12-PAB-(PEG4-Me)-Cit-Val-PEG2-amide-C2-MC
  • HY-131085
    Desmethyl Vc-seco-DUBA
    Desmethyl Vc-seco-DUBA consists a cleavable ADC linker (Desmethyl Vc-seco) and a DNA alkylating agent (DUBA). Desmethyl Vc-seco-DUBA can be used in the synthesis of antibody-drug conjugates (ADCs).
    Desmethyl Vc-seco-DUBA
Drug-Linker Conjugates for ADC Isoform Comparison

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