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-15578G
    McMMAF (GMP)
    McMMAF GMP is a GMP grade McMMAF (HY-15578). McMMAF is a protective group (maleimidocaproyl)-conjugated MMAF, which is a potent tubulin polymerization inhibitor. McMMAF can be used as a agent-linker for antibody-drug conjugates (ADC). McMMAF is uncleavable, and must be internalized and degraded within a cell, releasing cysteine-McMMAF as the active agent.
    McMMAF (GMP)
  • HY-145736A
    β-Glucuronide-dPBD-PEG5-NH2 TFA
    β-Glucuronide-dPBD-PEG5-NH2 TFA is the β-glucuronide-linked pyrrolobenzodiazepine dimer, which binds to the prenylated antibody for synthesis of antibody-drug conjugate (ADC) cIRCR201-dPBD.β-glucuronide-linkage as a cleavable linker. β-Glucuronide-dPBD-PEG5-NH2 TFA, as a proagent of cIRCR201-dPBD, reduces side effects. β-Glucuronide-dPBD-PEG5-NH2 TFA can induce apoptosis and arrest cell cycle. β-Glucuronide-dPBD-PEG5-NH2 TFA has antitumor activity.
    β-Glucuronide-dPBD-PEG5-NH2 TFA
  • HY-145736
    β-Glucuronide-dPBD-PEG5-NH2
    β-Glucuronide-dPBD-PEG5-NH2 is the β-glucuronide-linked pyrrolobenzodiazepine dimer, which binds to the prenylated antibody for synthesis of antibody-drug conjugate (ADC) cIRCR201-dPBD. β-glucuronide-linkage as a cleavable linker. β-Glucuronide-dPBD-PEG5-NH2, as a proagent of cIRCR201-dPBD, reduces side effects. β-Glucuronide-dPBD-PEG5-NH2 can induce apoptosis and arrest cell cycle. β-Glucuronide-dPBD-PEG5-NH2 has antitumor activity.
    β-Glucuronide-dPBD-PEG5-NH2
  • HY-148812
    Gly-Mal-Gly-Gly-Phe-Gly-amide-methylcyclopropane-Exatecan
    Gly-Mal-Gly-Gly-Phe-Gly-amide-methylcyclopropane-Exatecan is used for ADC Synthesis.
    Gly-Mal-Gly-Gly-Phe-Gly-amide-methylcyclopropane-Exatecan
  • HY-178290
    MC-Gly-Gly-Phe-Exatecan analog 38
    MC-Gly-Gly-Phe-Exatecan analog 38 (Compound L-II-4) is part of an antibody-drug conjugate (ADC), consisting of an ADC toxicant molecule and an ADC linker. MC-Gly-Gly-Phe-Exatecan analog 38 can be used to synthesize ADCs (such as ADC-II-15 and ADC-III-13). MC-Gly-Gly-Phe-Exatecan analog 38 can also be used in cancer research (ADC Cytotoxin: HY-178315, ADC Linker: HY-44235).
    MC-Gly-Gly-Phe-Exatecan analog 38
  • HY-164310
    TCO-PEG3-Glu-Val-Cit-PABC-MMAF
    TCO-PEG3-Glu-Val-Cit-PABC-MMAF is a linker-drug conjugate, which is consisted of a click pair TCO, a spacer PEG, a cleavable linker Glu-Val-Cit, a PBAC group and a cytotoxin MMAF (HY-15579). TCO-PEG3-Glu-Val-Cit-PABC-MMAF can be used for synthesis of dual drug ADC.
    TCO-PEG3-Glu-Val-Cit-PABC-MMAF
  • 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 (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-177541
    Ledadotin
    Ledadotin is a drug-linker conjugate for ADC. Ledadotin consists of a Microtubule inhibitor (Auristatin F-hydroxypropylamide) (HY-P5191) and a linker (BCN-PEG2-Gly-NH-tri(βAla-GGGG-Ser(mPEG8)-βAla-γGlu-Ala)) (HY-177562). Ledadotin can be used for synthesis of ADC Emiltatug ledadotin (HY-177542).
    Ledadotin
  • HY-178217
    JSSW-001
    JSSW-001 is a drug-linker compound applicable for the preparation of antibody-drug conjugates (ADCs). JSSW-001 can be used for the study of cancer.
    JSSW-001
  • HY-153908
    SMP-93566
    SMP-93566 is a kind of antibody-drug conjugates (ADCs) with a low payload shedding rate and has in vivo tumor inhibitory effects on ovarian cancer, gastric cancer, and breast cancer.
    SMP-93566
  • HY-171126
    DM21-L-G
    DM21-L-G is a Drug-Linker Conjugates that can be used to synthesize ADC molecules.
    DM21-L-G
  • HY-145951
    Amidate-VC-PAB-MMAF
    Amidate-VC-PAB-MMAF consists a cleavable ADC linker (Amidate-VC-PAB) and a potent tubulin polymerization inhibitor (MMAF). Amidate-VC-PAB-MMAF can be used in the synthesis of antibody-drug conjugates (ADCs). Amidate-VC-PAB-MMAF reduces off-target cytotoxicity of ADCs.
    Amidate-VC-PAB-MMAF
  • HY-153907
    SMP-88480
    SMP-88480 is an Antibody-Drug Conjugates (ADCs). SMP-88480 is stable in mouse, monkey and human plasma and has in vivo tumor inhibitory effects on ovarian cancer, gastric cancer, and breast cancer.
    SMP-88480
  • HY-170865
    OncoFAP-GlyPro-MMAF
    OncoFAP-GlyPro-MMAF is a Drug-Linker Conjugate for ADC with potent antitumor activity. OncoFAP-GlyPro-MMAF consists of Monomethylauristatin F (HY-15579) and a linker. OncoFAP-GlyPro-MMAF can be used for synthesis of ADCs.
    OncoFAP-GlyPro-MMAF
  • HY-156691
    TLR7/8 agonist 4 hydroxy-PEG6-acid
    TLR7/8 agonist 4 hydroxy-PEG6-acid is a drug-linker conjugates for ADC. TLR7/8 agonist 4 hydroxy-PEG6-acid consists of TLR7/8 agonist 4 (HY-139017) and a non-cleavable linker Hydroxy-PEG6-acid (HY-133050), and can be used for synthesis of ADCs.
    TLR7/8 agonist 4 hydroxy-PEG6-acid
  • HY-145078
    PNU-EDA-Gly5
    PNU-EDA-Gly5 is an oligo-glycine linker-payload for ADC synthesis, composed of a DNA topoisomerase I inhibitor PNU-159682 and a linker EDA-Gly5.
    PNU-EDA-Gly5
  • HY-169324
    APL-1092
    APL-1092 (Mal-Exo-EEVC-Exatecan) is a drug-linker conjugate for ADC, which contains Exatecan (HY-13631) (ADC payload) and a linker.
    APL-1092
  • HY-136289
    MB-VC-MGBA
    MB-VC-MGBA is a agent-linker conjugate for ADC with potent antitumor activity by using MGBA (minor-groove-binding DNA-alkylating agent), linked via the ADC linker MB-VC.
    MB-VC-MGBA
  • HY-178145
    Mc-Lys(PEG12)-Cap-Ala-Ala-PABC-exatecan
    Mc-Lys(PEG12)-Cap-Ala-Ala-PABC-exatecan (compound 12) is a Drug-Linker Conjugate for ADC. Mc-Lys(PEG12)-Cap-Ala-Ala-PABC-exatecan contains the ADC linker (Mc-Lys(PEG12)-Cap-Ala-Ala-PABC) (HY-178146) and a DNA topoisomerase I inhibitor Exatecan (HY-13631). Mc-Lys(PEG12)-Cap-Ala-Ala-PABC-exatecan can be used for the development of ADC targeting HER2-positive breast cancer.
    Mc-Lys(PEG12)-Cap-Ala-Ala-PABC-exatecan
  • HY-136291
    Sulfo-SPDB-DGN462
    Sulfo-SPDB-DGN462 is a agent-linker conjugate for ADC. Sulfo-SPDB-DGN462 consists a toxin DGN462 (HY-101150) conjugated to the cleavable Sulfo-SPDB linker. DGN462, a potent DNA-alkylating agent, shows anti-tumor activity, such as acute myeloid leukemia (AML).
    Sulfo-SPDB-DGN462
Drug-Linker Conjugates for ADC Isoform Comparison

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