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-169322
    APL-1081
    APL-1081 (Mal-Exo-EVC-MMAE) is part of an antibody-conjugated active molecule (ADC). APL-1081 is conjugated with an ADC linker (peptide Mal-Exo-EEVC) and a potent tubulin polymerization inhibitor, MMAE (HY-15162).
    APL-1081
  • HY-157813
    2-MSP-5-HA-GGFG-NH-CH2-O-CH2-CO-Exatecan
    		98.27%
    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-164088
    DBM-C5-VC-PAB-MMAE
    DBM-C5-VC-PAB-MMAE (Compound 3a) is a Drug-Linker conjugate for ADC. DBM-C5-VC-PAB-MMAE is composed of a linker C5-VC-PAB with a maleimide group DBM and an ADC toxin MMAE (HY-15162).
    DBM-C5-VC-PAB-MMAE
  • HY-W190943
    Azido-PEG4-Val-Cit-PAB-MMAE
    		99.43%
    Azido-PEG4-Val-Cit-PAB-MMAE is a agent-linker conjugate for ADC by using the anti-mitotic agent, monomethyl auristatin E (MMAE, a tubulin inhibitor), linked via the cleavable linker Azido-PEG4-Val-Cit-PAB-OH. Azido-PEG4-Val-Cit-PAB-MMAE 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.
    Azido-PEG4-Val-Cit-PAB-MMAE
  • 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-128899
    MC-Val-Cit-PAB-Auristatin E
    MC-Val-Cit-PAB-Auristatin E is a agent-linker conjugate for ADC with potent antitumor activity by using Auristatin E (a cytotoxic tubulin modifier), linked via the ADC linker MC-Val-Cit-PAB.
    MC-Val-Cit-PAB-Auristatin E
  • HY-126532
    Fmoc-Val-Cit-PAB-Duocarmycin TM
    		99.44%
    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-112615
    NAMPT inhibitor-linker 1
    		98.08%
    NAMPT inhibitor-linker 1 is a agent-linker conjugates for ADC, composed of an NAMPT inhibitor as a payload, and a linker. ADC-3 consists of an NAMPT inhibitor-linker 1 and an anti-c-Kit monoclonal antibody, exihibits potent activity against c-Kit expressing cell lines such as GIST-T1 and NCI-H526 cells, with IC50s of <3 pM and 9 pM, respectively.
    NAMPT inhibitor-linker 1
  • HY-145989A
    Aminobenzenesulfonic auristatin E TFA
    		99.39%
    Aminobenzenesulfonic auristatin E TFA is a agent-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.
    Aminobenzenesulfonic auristatin E TFA
  • HY-147095A
    Val-Ala-PABC-Exatecan trifluoroacetate
    		98.39%
    Val-Ala-PABC-Exatecan trifluoroacetate 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 trifluoroacetate can be used for ADC molecues synthesis, such as Mal-PEGn-amide-va-Exatecan.
    Val-Ala-PABC-Exatecan trifluoroacetate
  • 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-160157
    IM-2
    IM-2 is an ADC linker used in the synthesis of antibody-drug conjugates (ADCs).
    IM-2
  • HY-160774
    Val-Cit-PABC-DOX
    Val-Cit-PABC-DOX (compound 10109), an epsilon-poly-L-lysine-based drug conjugate, is an agent-linker conjugate for ADC by using a DNA topoisomerase I and topoisomerase II inhibitor, Doxorubicin (HY-15142), linked via the linker, Val-Cit-PABC.
    Val-Cit-PABC-DOX
  • HY-160807
    DBM-GGFG-NH-O-CO-Exatecan
    DBM-GGFG-NH-O-CO-Exatecan is an inhibitor for topoisomerase I. DBM-GGFG-NH-O-CO-Exatecan can be used as a drug-linker conjugate for synthesis of ADC molecule.
    DBM-GGFG-NH-O-CO-Exatecan
  • HY-164788
    GGFG-PAB-MMAE
    GGFG-PAB-MMAE (Comp 58054-1) is a drug-linker conjugate for ADC. GGFG-PAB-MMAE contains the ADC linker (GGFG-PAB) and a potent tubulin polymerization inhibitor MMAE (HY-15162).
    GGFG-PAB-MMAE
  • HY-W591408
    DBCO-Val-Cit-PAB-MMAE
    		98.33%
    DBCO-Val-Cit-PAB-MMAE is a drug-linker conjugate, which can be used for the synthesis of ADC molecules. MMAE (HY-15162) is a tubulin inhibitor, which can be used as an ADC toxin. DBCO-Val-Cit-PAB is the linker with the electrophilic group.
    DBCO-Val-Cit-PAB-MMAE
  • HY-160649
    MC-Gly-Gly-Phe-Gly-GABA-Exatecan
    		99.72%
    MC-Gly-Gly-Phe-Gly-GABA-Exatecan is an agent linker conjugate for ADC, with an inhibitor for Topoisomerase Exatecan (HY-13631) with IC50 of 22 μM. MC-Gly-Gly-Phe-Gly-GABA-Exatecan targets various antibodies, exhibits cytotoxic and antitumor efficacy in vitro and in vivo.
    MC-Gly-Gly-Phe-Gly-GABA-Exatecan
  • HY-170512
    Mal-GGFG-PAB-MMAE
    		99.96%
    Mal-GGFG-PAB-MMAE (Compound 8) is a drug-linker conjugate, which is composed of the mitotic inhibitor MMAE (HY-15162) and the linker Mal-GGFG-PAB. Mal-GGFG-PAB-MMAE can be used for synthesis of antibody-drug conjugate.
    Mal-GGFG-PAB-MMAE
  • HY-19697
    Aminocaproyl-Val-Cit-PABC-MMAE
    		99.89%
    Aminocaproyl-Val-Cit-PABC-MMAE is an Drug-linker conjugate for ADC.
    Aminocaproyl-Val-Cit-PABC-MMAE
  • HY-156758
    Mal-PEG8-Val-Cit-PAB-MMAF
    Mal-PEG8-Val-Cit-PAB-MMAF is a drug-linker conjugate for ADC. Mal-PEG8-Val-Cit-PAB-MMAF contains a cleavable ADC linker and a potent tubulin inhibitor MMAE (HY-15162).
    Mal-PEG8-Val-Cit-PAB-MMAF
Drug-Linker Conjugates for ADC Isoform Comparison

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