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

Drug-Linker Conjugates for ADC

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.

Cat. No. Product Name Effect Purity
  • HY-15575
    VcMMAE (mc-vc-PAB-MMAE) is a drug-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).
  • HY-13631E
    Deruxtecan is an ADC drug-linker conjugate composed of a derivative of DX-8951 (DXd) and a maleimide-GGFG peptide linker, used for synthesizing DS-8201 and U3-1402.
  • 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.
  • HY-128946
    CL2A-SN-38 is a drug-linker conjugate composed of a potent a DNA Topoisomerase I inhibitor SN-38 and a linker CL2A to make antibody drug conjugate (ADC). CL2A-SN-38 provides significant and specific antitumor effects against a range of human solid tumor types. CL2A is a nonclaevable complicated PEG8- and triazole-containing PABC-peptide-mc linker. CL2A is cleavable through pH sensitivity, giving rise to bystander effect, and binds the antibody at a cysteine residue via a disulfide bond.
  • HY-101070
    SMCC-DM1 (DM1-SMCC) is a drug-linker conjugate composed of a potent microtubule-disrupting agent DM1 and a linker SMCC to make antibody drug conjugate (ADC).
  • HY-145929
    MC-Val-Cit-PAB-Exatecan (MC-Val-Cit-PAB-DX8951) is a drug-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.
  • HY-147239
    MC-VA-PABC-MMAE is a drug-linker conjugate for ADC. MC-VA-PABC-MMAE contains the ADCs linker (peptide MC-VA-PABC) and a potent tubulin polymerization inhibitor MMAE (HY-15162).
  • HY-145989A
    Aminobenzenesulfonic auristatin E TFA
    Aminobenzenesulfonic auristatin E TFA is a drug-linker conjugate for ADC. Aminobenzenesulfonic auristatin E TFA has potent antitumor activity by using Auristatin E (a cytotoxic tubulin modifier), linked via the ADC linker Aminobenzenesulfonic.
  • HY-15578
    McMMAF is a protective group-conjugated MMAF. MMAF is a potent tubulin polymerization inhibitor.
  • HY-112786
    MC-Val-Cit-PAB-MMAF (Vc-MMAF) is a drug-linker conjugate for ADC with antitumor activity by using the tubulin inhibitor, MMAF, linked via cathepsin cleavable MC-Val-Cit-PAB.
  • HY-12460
    SPDB-DM4 is a drug-linker conjugate for ADC by using the maytansinebased payload (DM4, a tubulin inhibitor) via a SPDB linker, exhibiting potent anti-tumor activity.
  • HY-114233
    MC-GGFG-Exatecan (MC-GGFG-DX8951) is a drug-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).
  • HY-128952
    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.
  • HY-100374
    Val-Cit-PAB-MMAE is a drug-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.
  • HY-15741
    Mc-MMAE is a protective group (maleimidocaproyl)-conjugated monomethyl auristatin E (MMAE), which is a potent tubulin inhibitor. Mc-MMAE is a drug-linker conjugate for ADC.
  • HY-131057
    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).
  • HY-101162
    SGD-1910 is a drug-linker conjugate for ADC by using the antitumor antibiotic, pyrrolobenzodiazepine (PBD, a cytotoxic DNA crosslinking), linked via the cleavable linker MC-Val-Ala.
  • HY-126350
    CL2-SN-38 is a cleavable linker-based Drug-Linker conjugate, it can conjugate with the anti-Trop-2-humanized antibody hRS7. CL2-SN-38 can be used for the reasearch of cancer.
  • HY-111012
    DBCO-(PEG)3-VC-PAB-MMAE is made by MMAE conjugated to DBCO-(PEG)3-vc-PAB linker. Monomethyl auristatin E (MMAE), a potent tubulin inhibitor, is a toxin payload in antibody drug conjugate.
  • HY-116063
    Doxorubicin-SMCC is a drug-linker conjugate for ADC. Doxorubicin-SMCC contains a non-cleavable ADC linker and a DNA topoisomerase II inhibitor Doxorubicin.

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