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-13631E
    Deruxtecan
    		99.94%
    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
  • HY-15575
    VcMMAE
    		99.97%
    VcMMAE (mc-vc-PAB-MMAE) is a agent-linker conjugate for ADC with potent antitumor activity by using the anti-mitotic agent, monomethyl auristatin E (MMAE, a tubulin inhibitor), linked via the lysosomally cleavable dipeptide, valine-citrulline (vc).
    VcMMAE
  • HY-117410
    Vipivotide tetraxetan
    		Inhibitor 99.57%
    Vipivotide tetraxetan (PSMA-617) is a high potent prostate-specific membrane antigen (PSMA) inhibitor, with a Ki of 0.37 nM. Vipivotide tetraxetan (PSMA-617) is designed consisting of three components: the pharmacophore Glutamate-urea-Lysine, the chelator DOTA able to complex both 68Ga or 177Lu, and a linker connecting these two entities. Glutamate-urea-Lysine is the selective pharmacophore to bind to prostate specific membrane antigen.
    Vipivotide tetraxetan
  • HY-128946
    CL2A-SN-38
    		99.07%
    CL2A-SN-38 is a agent-linker conjugate composed of a potent a DNA Topoisomerase I inhibitor SN-38 and a linker CL2A to make antibody agent conjugate (ADC). CL2A-SN-38 provides significant and specific antitumor effects against a range of human solid tumor types. CL2A-SN-38 uses hydrolyzable linker to deliver active agents within tumor cells and in the tumor microenvironment, resulting in bystander effects.
    CL2A-SN-38
  • HY-100374
    Val-Cit-PAB-MMAE
    		99.83%
    Val-Cit-PAB-MMAE is a agent-linker conjugate for ADC. Val-Cit-PAB-MMAE contains the ADCs linker (peptide Val-Cit-PAB) and a potent tubulin inhibitor MMAE (HY-15162). MMAE a potent mitotic inhibitor by inhibiting tubulin polymerization.
    Val-Cit-PAB-MMAE
  • HY-164239
    NH2-PEG3-VC-PAB-MMAE
    		99.10%
    NH2-PEG3-VC-PAB-MMAE is a drug-linker conjugate for ADC, consisting of a cleavable ADC linker (NH2-PEG3-VC-PAB) and a potent tubulin inhibitor Monomethyl auristatin E (MMAE) (HY-15162). NH2-PEG3-VC-PAB-MMAE can be used in the synthesis of antibody-drug conjugates (ADCs).
    NH2-PEG3-VC-PAB-MMAE
  • HY-164792
    DBCO-PEG3-VC-Exatecan
    DBCO-PEG3-VC-Exatecan (compound 25) is a Drug-Linker Conjugate for ADC. DBCO-PEG3-VC-Exatecan contains the ADC linker (DBCO-PEG3-VC) and a DNA topoisomerase I inhibitor Exatecan (HY-13631).
    DBCO-PEG3-VC-Exatecan
  • HY-156848
    Fmoc-GGFG-DXd
    		99.81%
    Fmoc-GGFG-DXd is a drug-linker conjugate for ADC. Fmoc-GGFG-DXd contains a ADC linker Fmoc-GGFG and a DNA topoisomerase I inhibitor DXd (HY-13631D).
    Fmoc-GGFG-DXd
  • HY-15578
    McMMAF
    		99.96%
    McMMAF (Maleimidocaproyl monomethylauristatin F) is a maleimido-caproyl linker, made by coupling the powerful microtubule inhibitor Monomethyl auristatin F (MMAF) with the protecting group maleimidocaproyl. McMMAF serves as an active molecule linker for ADC. McMMAF is non-cleavable and must be internalized and degraded within the cell to release cysteine-McMMAF as the active molecule. McMMAF can be conjugated with anti-BCMA antibodies to form J6M0-mcMMAF, promoting apoptosis and inhibiting tumor growth.
    McMMAF
  • HY-101070
    SMCC-DM1
    		99.23%
    SMCC-DM1 (DM1-SMCC) is a agent-linker conjugate composed of a potent microtubule-disrupting agent DM1 and a linker SMCC to make antibody agent conjugate (ADC).
    SMCC-DM1
  • HY-114233
    MC-GGFG-Exatecan
    		99.71%
    MC-GGFG-Exatecan (MC-GGFG-DX8951) is a agent-linker conjugate for ADC. MC-GGFG-Exatecan is a DX8951 (a DNA topoisomerase I inhibitor) derivative with protease cleavable MC-GGFG linker. MC-GGFG-Exatecan shows antitumor activity and can be used to prepare DX8951 antibody conjugate (ADC).
    MC-GGFG-Exatecan
  • HY-112786
    MC-Val-Cit-PAB-MMAF
    		98.16%
    MC-Val-Cit-PAB-MMAF (Vc-MMAF) is a drug-linker conjugate for ADC by using the tubulin inhibitor, MMAF (HY-15579), linked via cathepsin cleavable MC-Val-Cit-PAB (HY-78738). MC-Val-Cit-PAB-MMAF shows antitumor activity.
    MC-Val-Cit-PAB-MMAF
  • HY-136314
    DBCO-PEG4-VC-PAB-MMAE
    		99.88%
    DBCO-PEG4-VC-PAB-MMAE consists a ADC linker (DBCO-PEG4-VC-PAB) and a tubulin polymerization inhibitor MMAE (HY-15162). DBCO-PEG4-VC-PAB-MMAE can be used in the synthesis of antibody-agent conjugates (ADCs). MMAE is a synthetic derivative of dolastatin 10 and functions as a potent mitotic inhibitor by inhibiting tubulin polymerization. DBCO-PEG4-VC-PAB-MMAE is a click chemistry reagent, it contains a DBCO group that can undergo strain-promoted alkyne-azide cycloaddition (SPAAC) with molecules containing Azide groups.
    DBCO-PEG4-VC-PAB-MMAE
  • HY-128952
    Tesirine
    		98.10%
    Tesirine (SG3249) is an antibody-drug conjugate (ADC) pyrrolobenzodiazepine (PBD) dimer payload. Tesirine combines potent antitumor activity with desirable physicochemical properties such as favorable hydrophobicity and improved conjugation characteristics. SG3199 (HY-101161) is the released warhead component of the ADC payload Tesirine. SG3199 retains picomolar activity in a panel of cancer cell lines. PBD dimers are highly efficient DNA minor groove cross-linking agents with potent cytotoxicity.
    Tesirine
  • HY-145929
    MC-Val-Cit-PAB-Exatecan
    MC-Val-Cit-PAB-Exatecan (MC-Val-Cit-PAB-DX8951) is a agent-linker conjugate for ADC. MC-Val-Cit-PAB-Exatecan is composed of a DNA topoisomerase I DX-8951 (HY-13631) and a cathepsin cleavable ADC linker.
    MC-Val-Cit-PAB-Exatecan
  • HY-134723
    DBCO-PEG4-GGFG-Dxd
    		98.42%
    DBCO-PEG4-GGFG-Dxd is a agent-linker conjugate for ADC with potent antitumor activity by using Dxd (a DNA topoisomerase I inhibitor), linked via the cleavable ADC linker DBCO-PEG4-GGFG. DBCO-PEG4-GGFG-Dxd is a click chemistry reagent, it contains a DBCO group that can undergo strain-promoted alkyne-azide cycloaddition (SPAAC) with molecules containing Azide groups.
    DBCO-PEG4-GGFG-Dxd
  • HY-12460
    SPDB-DM4
    		98.35%
    SPDB-DM4 is a agent-linker conjugate for ADC by using the maytansinebased payload (DM4, a tubulin inhibitor) via a SPDB linker, exhibiting potent anti-tumor activity.
    SPDB-DM4
  • HY-147270
    MC-VA-PAB-Exatecan
    		99.58%
    MC-VA-PAB-Exatecan is a agent-linker conjugate for ADC. MC-VA-PAB-Exatecan contains the ADC linker (peptide MC-VA-PAB) and a DNA topoisomerase I inhibitor Exatecan (HY-13631). MC-VA-PAB-Exatecan synthesized ADC shows good antitumor activity.
    MC-VA-PAB-Exatecan
  • HY-131057
    Mc-VC-PAB-SN38
    Mc-VC-PAB-SN38 consists a cleavable ADC linker (Mc-VC-PAB) and a DNA topoisomerase I inhibitor (SN38). Mc-VC-PAB-SN38 can be used in the synthesis of antibody-drug conjugates (ADCs).
    Mc-VC-PAB-SN38
  • HY-145399
    AZ14170133
    		98.95%
    Mal-PEG8-amide-Val-Ala-(4-NH2)-Exatecan is a Drug-Linker Conjugates for ADC, which comprises a topoisomerase inhibitor and a linker for ligand unit connecting. Mal-PEG8-amide-Val-Ala-(4-NH2)-Exatecan can be used to synthesis antibody-drug conjugate (ADC).
    AZ14170133
Drug-Linker Conjugates for ADC Isoform Comparison

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