2. Signaling Pathways
  3. Antibody-drug Conjugate/ADC Related
  4. Drug-Linker Conjugates for ADC

Drug-Linker Conjugates for ADC

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-163487
    Puxitatug samrotecan drug-linker
    Puxitatug samrotecan drug-linker (AZD8205 drug-linker) is part of the anti-B7-H4 antibody-conjugated active molecule ADC (drug-linker conjugate for ADC). Puxitatug samrotecan drug-linker contains a degradable ADC linker and a topoisomerase I inhibitor Exatecan (HY-13631).
    Puxitatug samrotecan drug-linker
  • HY-148380
    Mal-PEG8-Phe-Lys-PAB-Exatecan
    Mal-PEG8-Phe-Lys-PAB-Exatecan (compound 15) is a agent-linker conjugate for ADC, composed of degradable linker Mal-PEG8-Phe-Lys-PAB and toxin molecule Exatecan (HY-13631) composition.
    Mal-PEG8-Phe-Lys-PAB-Exatecan
  • 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-148194
    SC239
    		99.97%
    SC239 is a cleavable 2-aminophenyl hemiasterlin agent-linker. SC239 can be as the agent-linker for ADC. SC239 is a click chemistry reagent, it contains a DBCO group that can undergo strain-promoted alkyne-azide cycloaddition (SPAAC) with molecules containing Azide groups.
    SC239
  • HY-153739
    N3-PEG3-VC-PAB-MMAF
    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
  • HY-148668A
    MC-Gly-Gly-Phe-Gly-(S)-Cyclopropane-Exatecan
    MC-Gly-Gly-Phe-Gly-(R)-Cyclopropane-Exatecan is a agent-linker conjugates for ADC, consisting Exatecan (HY-13631). Exatecan is a DNA Topoisomerase I inhibitor (IC50=2.2 μM).
    MC-Gly-Gly-Phe-Gly-(S)-Cyclopropane-Exatecan
  • 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-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-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-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-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 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-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-160909
    8K13-hz35-STING-D4-1203
    8K13-hz35-STING-D4-1203 is a STING agonist-linker conjugate for ADC.
    8K13-hz35-STING-D4-1203
  • HY-152916
    mp-dLAE-PABC-MMAE
    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
Drug-Linker Conjugates for ADC Isoform Comparison

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