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-112616
    NAMPT inhibitor-linker 2
    		99.35%
    NAMPT inhibitor-linker 2 is a agent-linker conjugates for ADC, composed of an NAMPT inhibitor as a payload, and a linker. ADC-4 consists of an NAMPT inhibitor-linker 2 and an anti-c-Kit monoclonal antibody, exihibits potent activity against c-Kit expressing cell lines such as GIST-T1 and NCI-H526, with IC50s of <7 pM and 40 pM, respectively.
    NAMPT inhibitor-linker 2
  • HY-15742
    Vc-MMAD
    		99.96%
    Vc-MMAD consists the ADCs linker (Val-Cit) and potent tubulin inhibitor (MMAD). Vc-MMAD is a agent-linker conjugate for ADC.
    Vc-MMAD
  • 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.
    Mal-Val-Ala-PAB-N(SO2Me)-Exatecan
  • HY-153031
    Val-Cit-PAB-Exatecan
    		99.79%
    Val-Cit-PAB-Exatecan (Val-Cit-PAB-DX8951) is a agent-linker conjugate for ADC. Val-Cit-PAB-Exatecan is composed of a DNA topoisomerase I DX-8951 (HY-13631) and a cathepsin cleavable ADC linker.
    Val-Cit-PAB-Exatecan
  • HY-148436
    Glucocorticoid receptor agonist-2 Ala-Ala-Mal
    		98.99%
    Glucocorticoid receptor agonist-2 Ala-Ala-Mal (compound 79) can be used to synthesize anti-inflammatory ADC molecules. Glucocorticoid receptor agonist-2 is an active reference for ABBV-3373.
    Glucocorticoid receptor agonist-2 Ala-Ala-Mal
  • HY-19813A
    mDPR-Val-Cit-PAB-MMAE TFA
    		99.51%
    mDPR-Val-Cit-PAB-MMAE TFA is a drug-linker conjugate for ADC (Drug-Linker Conjugates for ADC), consisting of a tubulin polymerization inhibitor MMAE (HY-15162) and an ADC linker (peptide Val-Cit- PAB) composition[1].
    mDPR-Val-Cit-PAB-MMAE TFA
  • HY-156748
    MC-PEG2-VA-PAB-Exatecan
    		99.61%
    MC-PEG2-VA-PAB-Exatecan (Compound DL-18) is a Drug-Linker Conjugates for ADC. MC-PEG2-VA-PAB-Exatecan consists of Exatecan (HY-13631) and a linker. MC-PEG2-VA-PAB-Exatecan can be used for synthesis of ADCs.
    MC-PEG2-VA-PAB-Exatecan
  • HY-148127
    TAM558
    		99.29%
    TAM558 is a payload molecule used for the synthesis of OMTX705. OMTX705 is a humanized anti-fibroblast-activating protein (FAP) antibody conjugated to the cytolysin TAM470 (HY-148128), with antitumor activity.
    TAM558
  • HY-44177
    Val-Cit-PAB-MMAF sodium
    		98.43%
    Val-Cit-PAB-MMAF sodium is a agent-linker conjugate for ADC. Val-Cit-PAB-MMAF sodium contains the ADCs linker (peptide Val-Cit-PAB) and a potent tubulin polymerization inhibitor MMAF (HY-15579)
    Val-Cit-PAB-MMAF sodium
  • HY-160015
    CB07-Exatecan
    		98.97%
    CB07-Exatecan is an ADC drug-Linker conjugate that can be used for the synthesis of ADCs. ADC conjugated with CB07-Exatecan and trastuzumab inhibits the growth of HER2-positive cancer cells. CB07-Exatecan can be used in cancer research.
    CB07-Exatecan
  • HY-147204
    Mc-Alanyl-Alanyl-Asparagine-PAB-MMAE
    		99.34%
    Mc-Alanyl-Alanyl-Asparagine-PAB-MMAE (compound S6) is a potent anticancer agent, which can be specific activated by tumor microenvironment. Mc-Alanyl-Alanyl-Asparagine-PAB-MMAE can suppress tumor growth in mice (extracted from patent CN104147612A).
    Mc-Alanyl-Alanyl-Asparagine-PAB-MMAE
  • HY-139909A
    CL2E-SN38 TFA
    		99.51%
    CL2E-SN-38 TFA, a highly releasable and structurally stable antibody-SN-38-conjugate, is a part of the antibody drug conjugate (ADC). SN-38, the active metabolite of Irinotecan from camptothecins, is an Topoisomerase I inhibitor.
    CL2E-SN38 TFA
  • HY-153601
    MC-VC-PAB-Cyclohexanediamine-Thailanstatin A
    MC-VC-PAB-Cyclohexanediamine-Thailanstatin A is a Spliceostatin (HY-16466) analog, and a drug-linker conjugates for ADC, consisting of ADC Cytotoxin Thailanstatin A (HY-129589) and cleavable ADC linker (MC-vc-PAB). MC-VC-PAB-Cyclohexanediamine-Thailanstatin A can be used for ADC synthesis.
    MC-VC-PAB-Cyclohexanediamine-Thailanstatin A
  • HY-104025
    SPB
    		98.20%
    SPB is a agent-linker conjugate for ADC with potent anti-inflammatory activity by using Xanthotoxol, linked via the ADC linker.
    SPB
  • HY-141536
    PSMA-ALB-56
    		98.92%
    PSMA-ALB-56 is a PSMA-targeting radioligand designed by combining the glutamate-urea PSMA-binding entity and an albumin binder.
    PSMA-ALB-56
  • HY-156377
    Biotin-PEG7-Maleimide
    		99.42%
    Biotin-PEG7-Maleimide is a biotinylation reagent that reacts with thiol groups (SH). Biotin-PEG7-Maleimide can be used as Drug-Linker Conjugates for ADCs.
    Biotin-PEG7-Maleimide
  • HY-132161
    MP-PEG4-Val-Lys-Gly-7-MAD-MDCPT
    		98.97%
    MP-PEG4-Val-Lys-Gly-7-MAD-MDCPT is a Camptothecin-linker compound extracted from patent WO2019195665A1, example 4-1. MP-PEG4-Val-Lys-Gly-7-MAD-MDCPT is a agent-linker conjugate for antibody-drug conjugate (ADC).
    MP-PEG4-Val-Lys-Gly-7-MAD-MDCPT
  • HY-126683
    Mal-C6-α-Amanitin
    		98.48%
    Mal-C6-α-Amanitin is a agent-linker conjugate for ADC with potent antitumor activity by using α-Amanitin (an RNA polymerase II inhibitor), linked via the ADC linker Mal-C6.
    Mal-C6-α-Amanitin
  • HY-126491
    SPP-DM1
    SPP-DM1 is a agent-linker conjugate for ADC with potent antitumor activity by using DM1 (a potent microtubule-disrupting agent), linked via the ADC linker SPP.
    SPP-DM1
  • HY-148067
    XMT-1519 conjugate-1
    		99.26%
    ΧΜΤ-1519 conjugate-1 (compound 31) is a linker for the HER-2 monoclonal antibody XMT-1519, which can be used to synthesize ADC and increase anti-tumor activity.
    XMT-1519 conjugate-1
Drug-Linker Conjugates for ADC Isoform Comparison

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