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-111555
    AmPEG6C2-Aur0131
    AmPEG6C2-Aur0131 is a agent-linker conjugate for ADC (anti-CXCR4 ADC) with potent antitumor activity by using Aur0131 (an auristatin microtubule inhibitor), linked via the non-cleavable linker AmPEG6C2.
    AmPEG6C2-Aur0131
  • HY-164656
    DOTA-tris(acid)-amido-PEG24-amido-PEG24-DSPE
    DOTA-tris(acid)-amido-PEG24-amido-PEG24-DSPE is a radionuclide conjugate (RDC), which is capable of binding to a radionuclide. RDC has the ability to specifically target biomolecules and can be used in medical imaging or therapy.
    DOTA-tris(acid)-amido-PEG24-amido-PEG24-DSPE
  • HY-100374G
    Val-Cit-PAB-MMAE (GMP)
    Val-Cit-PAB-MMAE GMP is a GMP grade Val-Cit-PAB-MMAE (HY-100374). 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 (GMP)
  • HY-158348
    m-PEG8-Lys(Mal)-Val-Ala-PAB-Ph-CO-Dazostinag
    m-PEG8-Lys(Mal)-Val-Ala-PAB-Ph-CO-Dazostinag is a drug-linker conjugate for ADC.
    m-PEG8-Lys(Mal)-Val-Ala-PAB-Ph-CO-Dazostinag
  • HY-126689
    Mal-Phe-C4-VC-PAB-DMEA-PNU-159682
    Mal-Phe-C4-VC-PAB-DMEA-PNU-159682, a agent-linker conjugate for ADC, consists the ADC linker Mal-Phe-C4-VC-PAB and a potent ADC cytotoxin DMEA-PNU-159682. DMEA-PNU-159682 includes metabolites of nemorubicin (MMDX) from liver microsomes and ADC cytotoxin PNU-159682.
    Mal-Phe-C4-VC-PAB-DMEA-PNU-159682
  • HY-171125
    Maytansine derivative M24
    Maytansine derivative M24 is an ADC Drug-Linker Conjugates for ADC that can be used to synthesize ADC REGN5093-M114.
    Maytansine derivative M24
  • HY-164309
    DBCO-PEG3-Glu-Val-Cit-PABC-MMAE
    DBCO-PEG3-Glu-Val-Cit-PABC-MMAE is a drug-linker conjugate for ADC. DBCO-PEG3-Glu-Val-Cit-PABC-MMAE contains a potent tubulin inhibitor Monomethyl auristatin E (MMAE, HY-15162) and can be used for synthesis of dual-drug ADC.
    DBCO-PEG3-Glu-Val-Cit-PABC-MMAE
  • HY-136313
    MC-VC-PAB-Tubulysin M
    MC-vc-PAB-Tubulysin M is a synthetic ADC drug-linker conjugate composed of the tubulin polymerization inhibitor Tubulysin M (an ADC Cytotoxin) (HY-N7053) and MC-vc-PAB (a cleavable ADC linker).
    MC-VC-PAB-Tubulysin M
  • HY-128951
    AMCC-DM1
    AMCC-DM1 is a drug-linker conjugate composed of a potent a tubulin inhibitor DM4 and a linker AMCC to make antibody drug conjugate. AMCC is a noncleavable linker.
    AMCC-DM1
  • HY-173634
    Mal((3S,3aR,6S,6aR)-Hexahydrofuro[3,2-b]furan-3,6-diamine-PEG12)-β-Glu-PAB-Exatecan
    Mal((3S,3aR,6S,6aR)-Hexahydrofuro[3,2-b]furan-3,6-diamine-PEG12)-β-Glu-PAB-Exatecan (LP1) is a drug-linker conjugate composed of a potent a DNA Topoisomerase I inhibitor Exatecan (HY-13631) and a linker Mal((3S,3aR,6S,6aR)-Hexahydrofuro[3,2-b]furan-3,6-diamine-PEG12)-β-Glu-PAB (HY-173635) to make antibody agent conjugate (ADC), AZD0516 (HY-173639).
    Mal((3S,3aR,6S,6aR)-Hexahydrofuro[3,2-b]furan-3,6-diamine-PEG12)-β-Glu-PAB-Exatecan
  • HY-169323
    APL-1091
    APL-1091 (Mal-Exo-EEVC-MMAE) is part of a Drug-linker conjugate for ADC. APL-1091 contains a Mal-Exo-EEVC (HY-169353) linker and MMAE (HY-15162) (Microtubule inhibitor). APL-1091 can be used for ADC synthesis.
    APL-1091
  • HY-155313
    β-Glucuronide-NB-bis[N(Me)-methyl ester]-MMAE
    β-Glucuronide-NB-bis[N(Me)-methyl ester]-MMAE (compound 20) is auristatins-glucuronide conjugate. Antitumor agent-122 shows in vitro antiproliferative activities against β-glucuronidase pretreated and untreated cancer cells with an IC50 value of 5.7 nM - 9.7 nM. Antitumor agent-122 shows potent antitumor efficacy in HCT-116 xenograft mouse model without inducing side effects.
    β-Glucuronide-NB-bis[N(Me)-methyl ester]-MMAE
  • HY-158137
    Val-Cit-PAB-DEA-Dxd
    Val-Cit-PAB-DEA-Dxd (compound 81) is a Drug-Linker Conjugates for ADC, which is composed of a linker and a toxic molecule Dxd (DNA topoisomerase I inhibitor). Val-Cit-PAB-DEA-Dxd can be used for ADC synthesis.
    Val-Cit-PAB-DEA-Dxd
  • HY-164707
    MC7
    MC7 is a drug-linker conjugate for ADC and can be used for ADC synthesis. The payload is a NAMPT inhibitor (HY-402237).
    MC7
  • HY-139325
    NHS-Modified MMAF
    NHS-Modified MMAF (WO2012143499A2, intermediat 210) is an intermediate which can be used for producing the anti-mesothelin binder-agent conjugates (ADCs).
    NHS-Modified MMAF
  • HY-136321
    MC-betaglucuronide-MMAE-2
    MC-betaglucuronide-MMAE-2 is a agent-linker conjugate for ADC with potent antitumor activity by using MMAE (a tubulin polymerization inhibitor), linked via the cleavable ADC linker MC-betaglucuronide.
    MC-betaglucuronide-MMAE-2
  • HY-149416
    Mal-PEG8-Val-Ala-PAB-SB-743921
    Mal-PEG8-Val-Ala-PAB-SB-743921 (Compound D7) is a Drug-Linker Conjugates for ADC. Mal-PEG8-Val-Ala-PAB-SB-743921 consists of KSP inhibitor SB-743921 (HY-14661) and a linker. Mal-PEG8-Val-Ala-PAB-SB-743921 can be used for synthesis of ADCs.
    Mal-PEG8-Val-Ala-PAB-SB-743921
  • HY-139957
    Mal-amido-PEG8-Val-Ala-PAB-SG3200
    Mal-amido-PEG8-Val-Ala-PAB-SG3200 is a conjugate for antibody-drug conjugate (ADC) (extracted from patent WO2016166300A1).
    Mal-amido-PEG8-Val-Ala-PAB-SG3200
  • HY-141148
    7-O-(Cbz-N-amido-PEG4)-paclitaxel
    7-O-(Cbz-N-amido-PEG4)-paclitaxel is a PEG-class Drug-linker conjugates for ADC, containing a paclitaxel moiety and a amino group. The amine group is reactive with carboxylic acids, activated NHS esters, carbonyls (ketone, aldehyde) etc. 7-O-(Cbz-N-amido-PEG4)-paclitaxel can be used in the synthesis of Antibody-Drug Conjugates (ADCs).
    7-O-(Cbz-N-amido-PEG4)-paclitaxel
  • HY-168285
    LE01
    LE01 is a drug-linker conjugate for ADC. LE01 contains a ADC linker and a DNA topoisomerase I inhibitor DXd (HY-13631D). LE01 can be used to synthesize HER2-targeting ADC (HER2-LE01).
    LE01
Drug-Linker Conjugates for ADC Isoform Comparison

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