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-112615
    NAMPT inhibitor-linker 1
    		99.27%
    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-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-111554
    AcLys-PABC-VC-Aur0101
    AcLys-PABC-VC-Aur0101 is a agent-linker conjugate for ADC (anti-CXCR4 ADC) with potent antitumor activity by using Aur0101 (an auristatin microtubule inhibitor), linked via the cleavable linker AcLys-PABC-VC.
    AcLys-PABC-VC-Aur0101
  • HY-156848
    Fmoc-GGFG-DXd
    		99.81%
    Fmoc-GGFG-DXd is a drug-linker conjugate for ADC. Fmoc-GGFG-DXd contains a ADC linker Fmoc-GGFG and a DNA topoisomerase I inhibitor DXd (HY-13631D).
    Fmoc-GGFG-DXd
  • HY-19813A
    mDPR-Val-Cit-PAB-MMAE TFA
    		98.36%
    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-139909A
    CL2E-SN38 TFA
    		99.26%
    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-131089
    MC-VC-PABC-C6-α-Amanitin
    		99.62%
    MC-VC-PABC-C6-α-Amanitin is a Drug-Linker Conjugates for ADC, consisting of an anticancer toxin alpha-Amanitin (HY-19610) and a MC-VC-PABC-C6 linker. Among them, alpha-Amanitin is a potent inhibitor of RNA polymerase IIα.
    MC-VC-PABC-C6-α-Amanitin
  • HY-176559
    LacNAc-VC-PAB-MMAE
    LacNAc-VC-PAB-MMAE is a component of an Antibody-Drug Conjugate (ADC). LacNAc-VC-PAB-MMAE is assembled onto the N-glycosylation site of Trastuzumab (HY-P9907) by WT Endo-S2.
    LacNAc-VC-PAB-MMAE
  • HY-171822
    Cys-MC-VC-PAB-MMAE
    		98.23%
    Cys-MC-VC-PAB-MMAE consists a cleavable ADC linker (Cys-MC-VC-PAB) and a potent tubulin inhibitor (MMAE). Cys-MC-VC-PAB-MMAE can be used in the synthesis of antibody-drug conjugates (ADCs).
    Cys-MC-VC-PAB-MMAE
  • HY-147204
    Mc-Alanyl-Alanyl-Asparagine-PAB-MMAE
    		99.82%
    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-128979
    Deruxtecan analog 2
    		99.56%
    Deruxtecan analog 2 (example 9 P3) is a Deruxtecan (HY-13631E) analog. Deruxtecan analog 2 is a agent-linker conjugate composed of Camptothecin (HY-16560) and a linker. Camptothecin (CPT) is a Topo I inhibitor with antineoplastic activity against colorectal, breast, lung and ovarian cancers. Deruxtecan analog 2 can be used for the preparation anti-FGFR2 ADC.
    Deruxtecan analog 2
  • HY-15740
    Mc-MMAD
    		98.39%
    Mc-MMAD is a protective group (maleimidocaproyl)-conjugated MMAD. MMAD is a potent tubulin inhibitor. Mc-MMAD is a agent-linker conjugate for ADC.
    Mc-MMAD
  • 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-148380A
    Mal-PEG8-Phe-Lys-PAB-Exatecan TFA
    		98.66%
    Mal-PEG8-Phe-Lys-PAB-Exatecan TFA is a agent-linker conjugate for ADC, composed of degradable linker Mal-PEG8-Phe-Lys-PAB and toxin molecule Exatecan (HY-13631).
    Mal-PEG8-Phe-Lys-PAB-Exatecan TFA
  • HY-44177
    Val-Cit-PAB-MMAF sodium
    		98.97%
    Val-Cit-PAB-MMAF sodium is a drug-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-148245
    OH-Glu-Val-Cit-PAB-MMAE
    		99.03%
    OH-Glu-Val-Cit-PAB-MMAE consists a cleavable ADC linker (OH-Glu-Val-Cit-PAB) and a potent tubulin inhibitor (MMAE). SuO-Glu-Val-Cit-PAB-MMAE can be used in the synthesis of antibody-drug conjugates (ADCs).
    OH-Glu-Val-Cit-PAB-MMAE
  • HY-141147
    7-O-(Amino-PEG4)-paclitaxel
    		99.8%
    7-O-(Amino-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-(Amino-PEG4)-paclitaxel can be used in the synthesis of Antibody-Drug Conjugates (ADCs).
    7-O-(Amino-PEG4)-paclitaxel
  • HY-13631EG
    Deruxtecan (GMP)
    Deruxtecan (GMP) (MC-GGFG-DXD (GMP)) is Deruxtecan (HY-13631E) in GMP grade. GMP-grade small molecules can be used as auxiliary reagents in cell therapy. Deruxtecan is an ADC drug-linker conjugate composed of an DX-8951 derivative (DXd) and a maleimide-GGFG peptide linker, used for synthesizing Trastuzumab deruxtecan (HY-138298A) and Patritumab deruxtecan (HY-P99813).
    Deruxtecan (GMP)
  • HY-128711
    MAL-di-EG-Val-Cit-PAB-MMAF
    		98.56%
    MAL-di-EG-Val-Cit-PAB-MMAF consists the ADCs linker (MAL-di-EG-Val-Cit-PAB) and potent tubulin polymerization blocker (MMAF, Monomethyl auristatin F).
    MAL-di-EG-Val-Cit-PAB-MMAF
Drug-Linker Conjugates for ADC Isoform Comparison

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