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-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.
    BAY 1135626
  • HY-128903
    MC-Val-Cit-PAB-carfilzomib iodide
    MC-Val-Cit-PAB-carfilzomib iodide is a agent-linker conjugate for ADC with potent antitumor activity by using carfilzomib (an irreversible proteasome inhibitor), linked via the ADC linker MC-Val-Cit-PAB.
    MC-Val-Cit-PAB-carfilzomib iodide
  • HY-160157
    IM-2
    IM-2 is an ADC linker used in the synthesis of antibody-drug conjugates (ADCs).
    IM-2
  • 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-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
  • HY-101982A
    (Rac)-Lys-SMCC-DM1
    		98.18%
    (Rac)-Lys-SMCC-DM1 ((Rac)-Lys-Nε-MCC-DM1) is the racemate of Lys-SMCC-DM1 (HY-101982). Lys-SMCC-DM1 is a linker-payload component that has the potential to inhibit tubulin polymerization. Lys-SMCC-DM1 is the active metabolite of T-DM1.
    (Rac)-Lys-SMCC-DM1
  • 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-128897
    MC-VC-PABC-DNA31
    		98.71%
    MC-VC-PABC-DNA31 is a agent-linker conjugate for ADC with potent antitumor activity by using DNA31 (a potent RNA polymerase inhibitor), linked via the ADC linker MC-VC-PABC.
    MC-VC-PABC-DNA31
  • 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-148346A
    STING agonist-20-Ala-amide-PEG2-C2-NH2 TFA
    		98.30%
    STING agonist-20-Ala-amide-PEG2-C2-NH2 (Compound 30b) TFA is an active scaffold comprising a stimulator of interferon genes (STING). STING agonist-20-Ala-amide-PEG2-C2-NH2 TFA can be used to synthesize immune-stimulating antibody conjugate (ISAC). STING agonist-20-Ala-amide-PEG2-C2-NH2 TFA can be used for the research of cancer.
    STING agonist-20-Ala-amide-PEG2-C2-NH2 TFA
  • HY-400770
    MC-GGFG-AM-(10Me-11F-Camptothecin) intermediate-1
    MC-GGFG-AM-(10Me-11F-Camptothecin) intermediate-1 (compound 19-2) is an intermediate for the synthesis of MC-GGFG-AM-(10Me-11F-Camptothecin) (HY-153360). Modifying groups can be added group. MC-GGFG-AM-(10Me-11F-Camptothecin) is a drug-linker conjugate used in the synthesis of ADCs.
    MC-GGFG-AM-(10Me-11F-Camptothecin) intermediate-1
  • 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-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-157407
    Cyclooctyne-O-amido-PEG4-VC-PAB-Gly-Gly-NH-O-CO-Exatecan
    Cyclooctyne-O-amido-PEG4-VC-PAB-Gly-Gly-NH-O-CO-Exatecan is a drug-linker conjugate for ADC (ADC Cytotoxin: Exatecan).
    Cyclooctyne-O-amido-PEG4-VC-PAB-Gly-Gly-NH-O-CO-Exatecan
Drug-Linker Conjugates for ADC Isoform Comparison

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