GLPBio

Signaling Pathways

Research Area, Signaling Pathways | GlpBio Life Science Products Suppliers

Read More about this category

The antibody-drug conjugate (ADC), a humanized or human monoclonal antibody conjugated with highly cytotoxic small molecules (payloads) through chemical linkers, is a novel therapeutic format and has great potential to make a paradigm shift in cancer chemotherapy. The three components of the ADC together give rise to a powerful oncolytic agent capable of delivering normally intolerable cytotoxins directly to cancer cells, which then internalize and release the cell-destroying drugs. At present, two ADCs, Adcetris and Kadcyla, have received regulatory approval with >40 others in clinical development.

ADCs are administered intravenously in order to prevent the mAb from being destroyed by gastric acids and proteolytic enzymes. The mAb component of the ADC enables it to circulate in the bloodstream until it finds and binds to tumor-specific cell surface antigens present on target cancer cells. Linker chemistry is an important determinant of the safety, specificity, potency and activity of ADCs. Linkers are designed to be stable in the blood stream (to conform to the increased circulation time of mAbs) and labile at the cancer site to allow rapid release of the cytotoxic drug. First generation ADCs made use of early cytotoxins such as the anthracycline, doxorubicin or the anti-metabolite/antifolate agent, methotrexate. Current cytotoxins have far greater potency and can be divided into three main groups: auristatins, maytansines and calicheamicins.

The development of site-specific conjugation methodologies for constructing homogeneous ADCs is an especially promising path to improving ADC design, which will open the way for novel cancer therapeutics.

References:

[1] Tsuchikama K, et al. Protein Cell. 2016 Oct 14. DOI:10.1007/s13238-016-0323-0.

[2] Peters C, et al. Biosci Rep. 2015 Jun 12;35(4). pii: e00225. doi: 10.1042/BSR20150089.

Research Areas

Products Related to Signaling Pathways(40698)

  • GC80971 structure
    GC80971N-Methylthalidomide
    CAS: 42472-93-5
    Purity: >98.00%

    N-Methylthalidomide is a cereblon ligand derivative that acts as an E3 ubiquitin ligase ligand for the synthesis of PROTAC LLC0424 N.

  • GC80972 structure
    GC80972Glutarimide-(1-oxoisoindoline-5-carbaldehyde)
    CAS: 2582979-82-4
    Purity: >97.00%

    Glutarimide-(1-oxoisoindoline-5-carbaldehyde) is an E3 ubiquitin ligase cereblon (CRBN) ligand used to recruit the cereblon protein.

  • GC80973 structure
    GC80973Desamino lenalidomide-5-CO
    CAS: 2866307-09-5
    Purity: >98.00%

    Desamino lenalidomide-5-CO is an E3 ubiquitin ligase cereblon (CRBN) ligand used to recruit the cereblon protein.

  • GC80974 structure
    GC80974C5 Lenalidomide-CH3
    CAS: 2768326-37-8
    Purity: >98.00%

    C5 Lenalidomide-CH3 is an E3 ubiquitin ligase cereblon (CRBN) ligand used to recruit the cereblon protein.

  • GC80975 structure
    GC80975(S)-Thalidomide 4-fluoride
    CAS: 911109-85-8
    Purity: >98.00%

    (S)-Thalidomide 4-fluoride is a CRBN E3 ligase ligand that can be used for synthesis of DeDPP4.

  • GC80976 structure
    GC80976CRBN ligand-661
    CAS: 2154343-24-3
    Purity: >96.50%

    CRBN ligand-661 is an E3 ubiquitin ligase cereblon (CRBN) ligand used to recruit the cereblon protein.

  • GC80977 structure
    GC80977CRBN ligand-788
    CAS: 2304753-45-3
    Purity: >98.00%

    CRBN ligand-788 is an E3 ubiquitin ligase cereblon (CRBN) ligand used to recruit the cereblon protein.

  • GC80978 structure
    GC809785,6-Difluoro-desamino lenalidomide
    CAS: 2438241-40-6
    Purity: >98.00%

    5,6-Difluoro-desamino lenalidomide is an E3 ubiquitin ligase cereblon (CRBN) ligand used to recruit the cereblon protein.

  • GC80979 structure
    GC80979CRBN ligand-789
    CAS: 2304754-82-1
    Purity: >98.00%

    CRBN ligand-789 is an E3 ubiquitin ligase cereblon (CRBN) ligand used to recruit the cereblon protein.

  • GC80980 structure
    GC80980Desamino lenalidomide-COOH
    CAS: 2287259-68-9
    Purity: >98.50%

    Desamino lenalidomide-COOH is an E3 ubiquitin ligase cereblon (CRBN) ligand used to recruit the cereblon protein.

  • GC80981 structure
    GC80981Desamino lenalidomide-6-COOH
    CAS: 2171780-01-9
    Purity: >98.00%

    Desamino lenalidomide-6-COOH is an E3 ubiquitin ligase cereblon (CRBN) ligand used to recruit the cereblon protein.

  • GC80982 structure
    GC80982Desamino lenalidomide-5-COOH
    CAS: 2171519-15-4
    Purity: >99.00%

    Desamino lenalidomide-5-COOH is an E3 ubiquitin ligase cereblon (CRBN) ligand used to recruit the cereblon protein.

  • GC80983 structure
    GC80983CRBN ligand-761
    CAS: 2925099-10-9
    Purity: >98.00%

    CRBN ligand-761 is an E3 ubiquitin ligase cereblon (CRBN) ligand used to recruit the cereblon protein.

  • GC80984 structure
    GC80984Desamino lenalidomide-NO2
    CAS: 1198787-23-3
    Purity: >99.50%

    Desamino lenalidomide-NO2 is an E3 ubiquitin ligase cereblon (CRBN) ligand used to recruit the cereblon protein.

  • GC80985 structure
    GC80985CRBN ligand-210
    CAS: 79987-78-3
    Purity: >98.00%

    CRBN ligand-210 is an E3 ubiquitin ligase cereblon (CRBN) ligand used to recruit the cereblon protein.

  • GC80986 structure
    GC80986CRBN ligand-397
    CAS: 2736511-32-1
    Purity: >98.50%

    CRBN ligand-397 is an E3 ubiquitin ligase cereblon (CRBN) ligand used to recruit the cereblon protein.

  • GC80987 structure
    GC80987CRBN ligand-750
    CAS: 2736510-38-4
    Purity: >98.00%

    CRBN ligand-750 is an E3 ubiquitin ligase cereblon (CRBN) ligand used to recruit the cereblon protein.

  • GC80988 structure
    GC80988CRBN ligand-890
    CAS: 2623101-33-5
    Purity: >96.50%

    CRBN ligand-890 is an E3 ubiquitin ligase cereblon (CRBN) ligand used to recruit the cereblon protein.

  • GC80989 structure
    GC80989Hydrouracil-(4-Br-2,6-difluorobenzene)
    CAS: 1499388-70-3
    Purity: >97.00%

    Hydrouracil-(4-Br-2,6-difluorobenzene) is an E3 ubiquitin ligase cereblon (CRBN) ligand used to recruit the cereblon protein.

  • GC80990 structure
    GC80990CRBN ligand-395
    CAS: 2641512-74-3
    Purity: >98.00%

    CRBN ligand-395 is an E3 ubiquitin ligase cereblon (CRBN) ligand used to recruit the cereblon protein.

  • GC80991 structure
    GC80991CRBN ligand-618
    CAS: 2713619-96-4
    Purity: >98.00%

    CRBN ligand-618 is an E3 ubiquitin ligase cereblon (CRBN) ligand used to recruit the cereblon protein.

  • GC80992 structure
    GC80992CRBN ligand-617
    CAS: 2713620-89-2
    Purity: >98.00%

    CRBN ligand-617 is an E3 ubiquitin ligase cereblon (CRBN) ligand used to recruit the cereblon protein.

  • GC80993 structure
    GC80993Desamino lenalidomide-CH2NH2 hydrochloride
    CAS: 2248702-12-5
    Purity: >95.00%

    Desamino lenalidomide-CH2NH2 hydrochloride is an E3 ubiquitin ligase cereblon (CRBN) ligand used to recruit the cereblon protein.

  • GC80994 structure
    GC80994CRBN ligand-394
    CAS: 2641512-77-6
    Purity: >99.50%

    CRBN ligand-394 is an E3 ubiquitin ligase cereblon (CRBN) ligand used to recruit the cereblon protein.