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-147095
    Val-Ala-PABC-Exatecan
    		98.19%
    Val-Ala-PABC-Exatecan is a Drug-Linker Conjugates for ADC，consiting of a cleavable Tesirine linker (Val-Ala-PABC) and Exatecan (topoisomerase I inhibitor，HY-13631). Val-Ala-PABC-Exatecan can be used for ADC molecues synthesis，such as Mal-PEGn-amide-va-Exatecan.
    Val-Ala-PABC-Exatecan
  • HY-160899A
    Thailanstatin A cyclohexane diamine formic
    Thailanstatin A cyclohexane diamine formic is an analog of Spliceostatin (HY-16466). Thailanstatin A cyclohexane diamine formic inhibits proliferations of cells N87 (IC50 is 0.33 μM), BT474 (IC50 is 0.34 μM), MDA-MB-361-DYT2 (IC50 is 0.88 μM) and MDA-MB-468 (IC50 is 0.27 μM). Thailanstatin A cyclohexane diamine formic is used as a drug-linker conjugate for ADC molecule.
    Thailanstatin A cyclohexane diamine formic
  • HY-15750
    Cys-mcMMAD
    		98.77%
    Cys-mcMMAD is a agent-linker conjugate for ADC. MMAD is a potent tubulin inhibitor.
    Cys-mcMMAD
  • 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.
    DM1-PEG4-DBCO
  • HY-139326
    NHS-MMAF
    NHS-MMAF is a modified MMAF extracted from patent WO2012143499, intermediat 219. MMAF is a potent tubulin polymerization inhibitor and is used as a antitumor agent
    NHS-MMAF
  • HY-141860
    PSMA-Val-Cit-PAB-MMAE
    		Inhibitor 99.52%
    PSMA-Val-Cit-PAB-MMAE is a novel small-molecule PSMA-targeted conjugate based on the monomethyl auristatin E for the chemotherapy of prostate cancer.
    PSMA-Val-Cit-PAB-MMAE
  • HY-136260
    DBCO-PEG4-Ahx-DM1
    DBCO-PEG4-Ahx-DM1 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. DBCO-PEG4-Ahx-DM1 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-Ahx-DM1
  • HY-126532
    Fmoc-Val-Cit-PAB-Duocarmycin TM
    		≥99.0%
    Fmoc-Val-Cit-PAB-Duocarmycin TM is a agent-linker conjugate for ADC by using the antitumor antibiotic, Duocarmycin TM, linked via Fmoc-Val-Cit-PAB.
    Fmoc-Val-Cit-PAB-Duocarmycin TM
  • HY-136297
    DGN549-C
    DGN549-C consists a cleavable ADC linker valine-alanine (va) and PBD dimer. DGN549 is a novel DNA-alkylating cytotoxic payload and can be used in the synthesis of antibody-agent conjugates (ADCs).
    DGN549-C
  • HY-128909
    MC-Val-Cit-PAB-rifabutin
    MC-Val-Cit-PAB-rifabutin is a agent-linker conjugate for ADC with potent antitumor activity by using rifabutin (an DNA-dependent RNA polymerase inhibitor), linked via the ADC linker MC-Val-Cit-PAB.
    MC-Val-Cit-PAB-rifabutin
  • HY-128906
    MC-Val-Cit-PAB-Retapamulin
    		99.00%
    MC-Val-Cit-PAB-Retapamulin is a agent-linker conjugate for ADC with potent antitumor activity by using Retapamulin (a ribosome inhibitor), linked via the ADC linker MC-Val-Cit-PAB.
    MC-Val-Cit-PAB-Retapamulin
  • HY-159072
    Mal-Val-Ala-PAB-N(SO2Me)-Exatecan
    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.
    Mal-Val-Ala-PAB-N(SO2Me)-Exatecan
  • HY-128908
    MC-Val-Cit-PAB-Indibulin
    MC-Val-Cit-PAB-Indibulin is a agent-linker conjugate for ADC with potent antitumor activity by using Indibulin (an orally applicable inhibitor of tubulin assembly), linked via the ADC linker MC-Val-Cit-PAB.
    MC-Val-Cit-PAB-Indibulin
  • HY-145989S
    Aminobenzenesulfonic auristatin E-d8
    		98.02%
    Aminobenzenesulfonic auristatin E-d8 is the deuterium labeled Aminobenzenesulfonic auristatin E. Aminobenzenesulfonic auristatin E is a drug-linker conjugate for ADC. Aminobenzenesulfonic auristatin E has potent antitumor activity by using Auristatin E (a cytotoxic tubulin modifier), linked via the ADC linker Aminobenzenesulfonic[1][2].
    Aminobenzenesulfonic auristatin E-d<sub>8</sub>
  • HY-15575S
    VcMMAE-d8
    VcMMAE-d8 is an isotope of VcMMAE (HY-15575). VcMMAE-d8 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-d<sub>8</sub>
  • HY-147286A
    Ac-Lys-Val-Cit-PABC-MMAE formic
    		99.96%
    Ac-Lys-Val-Cit-PABC-MMAE (formic) is a agent-linker conjugate for ADC. Ac-Lys-Val-Cit-PABC-MMAE contains the ADC linker (peptide Ac-Lys-Val-Cit-PABC) and a potent tubulin polymerization inhibitor auristatin E.html" class="link-product" target="_blank"> Monomethyl auristatin E (HY-15162).
    Ac-Lys-Val-Cit-PABC-MMAE formic
  • HY-156515
    MC-GGFG-(7ethanol-10NH2-11F-Camptothecin)
    MC-GGFG-(7ethanol-10NH2-11F-Camptothecin) (compound 141) is a drug-linker conjugates for ADC. MC-GGFG-(7ethanol-10NH2-11F-Camptothecin) is a MC-GGFG-(7ethanol-10NH2-11F-Camptothecin) with protease cleavable MC-GGFG linker.
    MC-GGFG-(7ethanol-10NH2-11F-Camptothecin)
  • HY-157813
    2-MSP-5-HA-GGFG-NH-CH2-O-CH2-CO-Exatecan
    2-MSP-5-HA-GGFG-NH-CH2-O-CH2-CO-Exatecan is a drug-linker conjugates for ADC, consiting of a cleavable linker and Exatecan (HY-13631). 2-MSP-5-HA-GGFG-NH-CH2-O-CH2-CO-Exatecan can be linked to anti-Her3 antibody.
    2-MSP-5-HA-GGFG-NH-CH2-O-CH2-CO-Exatecan
  • HY-128942
    MAC glucuronide α-hydroxy lactone-linked SN-38
    MAC glucuronide α-hydroxy lactone-linked SN-38 (Topoisomerase I inhibitor) is a stabilized lactone MAC glucuronide α-hydroxy lactone-linked SN-38 agent linker. MAC glucuronide α-hydroxy lactone-linked SN-38 is cytotoxic across L540cy cells and Ramos cells with IC50 values of 99 and 105 ng/mL, respectively.
    MAC glucuronide α-hydroxy lactone-linked SN-38
  • HY-126693
    SC-VC-PAB-DM1
    SC-VC-PAB-DM1 is a agent-linker conjugate for ADC with with potent antitumor activity by using DM1 (Mertansine, a tubulin inhibitor) , linked via the ADC linker SC-VC-PAB.
    SC-VC-PAB-DM1
Drug-Linker Conjugates for ADC Isoform Comparison

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