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-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-176765
    DBCO-PEG4-VA-PABC-MMAE
    DBCO-PEG4-VA-PABC-MMAE is a drug-linker conjugate for ADC. DBCO-PEG4-VA-PABC-MMAE consists of a tubulin inhibitor (MMAE) (HY-15162) and a cleavable linker (DBCO-PEG4-VA-PABC). DBCO-PEG4-VA-PABC-MMAE can be used for synthesis of ADC ABBV-400 (HY-171945).
    DBCO-PEG4-VA-PABC-MMAE
  • 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
  • HY-155744
    Acetylene-PEG3-MMAF-OMe
    Acetylene-PEG3-MMAF-OMe (LCB14-0536) is a protein-active agent conjugate. Acetylene-PEG3-MMAF-OMe can be recognized by isoprenoid transferase. Acetylene-PEG3-MMAF-OMe is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
    Acetylene-PEG3-MMAF-OMe
  • HY-164706
    m-PEG6-Lys-Mal-Toxophore-quinoline
    m-PEG6-Lys-Mal-Toxophore-quinoline is a drug-linker conjugate for ADC and can be used for ADC synthesis. The payload is a NAMPT inhibitor (HY-164760).
    m-PEG6-Lys-Mal-Toxophore-quinoline
  • HY-145365
    DGN549-L
    DGN549-L is a DNA alkylator and can be utilized for antibody conjugation at lysine residues. DGN549-L can be used in the synthesis of antibody-drug conjugates (ADCs).
    DGN549-L
  • HY-137774
    Clezutoclax
    Clezutoclax is a agent-linker conjugate for ADC . Clezutoclax can be used in the synthesis of antibody-drug conjugates (ADCs).
    Clezutoclax
  • HY-128961
    MC-Alkyl-Hydrazine Modified MMAF
    MC-Alkyl-Hydrazine Modified MMAF is a agent-linker conjugate for ADC with potent antitumor activity by using the Modified MMAF (a tubulin inhibitor), linked via the noncleavable MC-Alkyl-Hydrazine.
    MC-Alkyl-Hydrazine Modified MMAF
  • HY-158349
    Mal-Val-Ala-PAB-4-Abu(Me)-Dazostinag
    Mal-Val-Ala-PAB-4-Abu(Me)-Dazostinag is a drug-linker conjugate for ADC.
    Mal-Val-Ala-PAB-4-Abu(Me)-Dazostinag
  • HY-13631ES
    Deruxtecan-d4
    Deruxtecan-d4 is deuterium labeled Deruxtecan (HY-13631E). Deruxtecan is an ADC drug-linker conjugate composed of an DX-8951 derivative (DXd) and a maleimide-GGFG peptide linker, used for synthesizing DS-8201 and U3-1402.
    Deruxtecan-d<sub>4</sub>
  • HY-153069A
    GGFG-PAB-Exatecan TFA
    GGFG-PAB-Exatecan TFA consists of an ADC toxin Exatecan (HY-13631) and a linker GGFG-PAB, and can be used as a drug-linker conjugate for the synthesis of ADC molecules.
    GGFG-PAB-Exatecan TFA
  • HY-160756A
    Val-Cit-Exatecan TFA
    Val-Cit-Exatecan TFA is an agent-linker conjugate for ADC. Val-Cit-Exatecan TFA is composed of a DNA topoisomerase I Exatecan (HY-13631) and a cathepsin cleavable ADC linker.
    Val-Cit-Exatecan TFA
  • HY-145943
    MP-PEG8-Val-Lys-Ala-7-MAD-MDCPT
    MP-PEG8-Val-Lys-Ala-7-MAD-MDCPT is a agent-linker conjugate for antibody-drug conjugate (ADC). MP-PEG8-Val-Lys-Ala-7-MAD-MDCPT has the potential for cancer and autoimmune disease research.
    MP-PEG8-Val-Lys-Ala-7-MAD-MDCPT
  • HY-163673
    Glucocorticoid receptor modulator 4
    Glucocorticoid receptor modulator 4 (Compound DL5) is a conjugate of a linker and a glucocorticoid receptor modulator. Glucocorticoid receptor modulator 4 exhibits GRE Reporter activity in mTNF expressing K562 cell with an EC50 of 40 μM. Glucocorticoid receptor modulator 4 binds with an anti-tumor necrosis factor (TNF) antibody, and exhibits anti-inflammtory activity against arthritis in mouse models.
    Glucocorticoid receptor modulator 4
Drug-Linker Conjugates for ADC Isoform Comparison

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