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.

Drug-Linker Conjugates for ADC Related Products (341):

Cat. No. Product Name Effect Purity
  • HY-128946
    CL2A-SN-38
    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[1].
  • 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.
  • 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.
  • HY-117410
    Vipivotide tetraxetan Inhibitor 99.46%
    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.
  • HY-15575
    VcMMAE
    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).
  • HY-171508
    Mal-PNU-159682
    Mal-PNU-159682 is a Drug-Linker Conjugates for ADC, composes of ADC linker (maleimide) and ADC cytotoxin PNU-159682 (HY-16700), and has anti-tumor activity[1].
  • HY-171509
    Mal-N(Me)-C6-N(Me)-PNU-159682
    Mal-N(Me)-C6-N(Me)-PNU-159682 (Compound 27), an agent-linker conjugate for ADC, consists the ADC linker Mal-N(Me)-C6-N(Me) and a potent ADC cytotoxin PNU-159682. Mal-N(Me)-C6-N(Me)-PNU-159682 (Compound 27) selectively delivers the payload to CD46-expressing cells, where the linker is cleaved by cathepsin B to release PNU-159682, inducing DNA damage and apoptosis. Mal-N(Me)-C6-N(Me)-PNU-159682 shows durable tumor regression in xenograft (PDX) models of non-small cell lung cancer (NSCLC) and colorectal cancer (CRC)[1].
  • HY-171580
    Mc-PEG4-Val-Ala-PAB-Exatecan
    Mc-PEG4-Val-Ala-PAB-Exatecan is a Drug-linker conjugate for ADC. Mc-PEG4-Val-Ala-PAB-Exatecan contains the ADC linker (Mc-PEG4-Val-Ala-PAB) and a DNA topoisomerase I inhibitor Exatecan (HY-13631)[1].
  • HY-132158
    MC-AAA-NHCH2OCH2COO-7-aminomethyl-10-methyl-11-fluoro camptothecin
    MC-AAA-NHCH2OCH2COO-7-aminomethyl-10-methyl-11-fluoro camptothecin (compound 21a), a camptothecin payload, can be conjugated to a monoclonal antibody (mAb) for the synthesis of camptothecin antibody-drug conjugate (ADC)[1].
  • HY-101909
    Val-Cit-PAB-MMAF
    Val-Cit-PAB-MMAF is a agent-linker conjugate for ADC. Val-Cit-PAB-MMAF contains the ADCs linker (peptide Val-Cit-PAB) and a potent tubulin polymerization inhibitor MMAF (HY-15579)[1]
  • HY-159072
    Mal-Val-Ala-PAB-N(SO2Me)-Exatecan 98.00%
    Mal-Val-Ala-PAB-N(SO2Me)-Exatecan (Compound LE14) is a conjugate of an ADC toxin Exatecan (HY-13631) and a linker Mal-Val-Ala-PAB-N(SO2Me). Mal-Val-Ala-PAB-N(SO2Me)-Exatecan can be used for synthesis of ADC FZ-AD005. FZ-AD005 is a delta-like ligand 3 (DLL3, KD=58.3 pM) targeting ADC, that exhibits antitumor efficacy against SCLC cancer[1][2].
  • HY-141155
    endo-BCN-PEG4-Val-Cit-PAB-MMAE 99.95%
    endo-BCN-PEG4-Val-Cit-PAB-MMAE is a cleavable 4 unit PEG ADC linker used in the synthesis of antibody-drug conjugates (ADCs)[1]. endo-BCN-PEG4-Val-Cit-PAB-MMAE is a click chemistry reagent, it contains a BCN group that can undergo strain-promoted alkyne-azide cycloaddition (SPAAC) with molecules containing Azide groups.
  • HY-15750
    Cys-mcMMAD 98.77%
    Cys-mcMMAD is a agent-linker conjugate for ADC. MMAD is a potent tubulin inhibitor.
  • HY-147281
    BAY 1135626 99.19%
    BAY 1135626 is used to synthesize BAY 1129980, and use to anti-tumor research. BAY 1129980 is a Auristatin-based anti-C4.4A (LYPD3) antibody–agent conjugate (ADC), is used to non–small cell lung cancer (NSCLC) research[1].
  • 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[1]. 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.
  • HY-136261
    DM1-PEG4-DBCO 98.04%
    DM1-(PEG)4-DBCO is a agent-linker conjugate composed of a potent microtubulin inhibitor DM1 and a linker DBCO-PEG4-Ahx to make antibody agent conjugate (ADC). Mertansine (DM1) is a microtubulin inhibitor and is an antibody-conjugatable maytansinoid that is developed to overcome systemic toxicity associated with maytansine and to enhance tumor-specific delivery. DM1-PEG4-DBCO is a click chemistry reagent, it contains a DBCO group that can undergo strain-promoted alkyne-azide cycloaddition (SPAAC) with molecules containing Azide groups.
  • HY-147271
    Mal-PEG8-Val-Ala-PAB-Exatecan 99.48%
    Mal-PEG8-Val-Ala-PAB-Exatecan (Compound 9b) is an antibody-drug conjugate linker (ADC linker) that binds to Nectin-4 polypeptides conjugated to chemotherapeutic agents. Mal-PEG8-Val-Ala-PAB-Exatecan can be used for cancer research[1].
  • 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)[1].
  • HY-148426
    OSu-PEG4-VC-PAB-MMAE 98.91%
    OSu-PEG4-VC-PAB-MMAE involves in GDP-FAmP4MMAE (Monomethylauristatin E) synthesis, which is for GDP label via site-specific conjugation[1].
  • 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[1]. 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.