1. Signaling Pathways
  2. Antibody-drug Conjugate/ADC Related
  3. PROTAC-Linker Conjugates for PAC

PROTAC-Linker Conjugates for PAC

PROTAC-Linker for PROTAC-antibody Conjugates

PROTAC-linker Conjugate for PAC comprises an antibody conjugated via a linker to a PROTAC. The PROTAC-Antibody Conjugate (PAC) molecules comprise an antibody conjugated via a linker (L1) to a PROTAC, wherein the PROTAC comprises an ubiquitin E3 ligase binding groug (“E3LB”), a linker (“L2”) and a protein binding group (“PB”). To obtain a PAC having potent efficacy and a desirable therapeutic index, the following components are provided. 1. Antibody (Ab): The antibody portion of a PAC can target a cell that expresses an antigen whereby the antigen specific PAC is delivered intracellularly to the target cell, typically through endocytosis While PACs that comprise an antibody directed to an antigen that is not found on the cell surface may result in less specific intracellular delivery of the PROTAC portion into the cell, the PAC may still undergo pinocytosis. 2. Linkers (L1): A“linker” (L1) is a bifunctional or multifunctional moiety that can be used to link one or more PROTAC moieties (D) to an antibody (Ab) to form a PAC. In some embodiments, PACs can be prepared using a L1 having reactive functionalities for covalently attaching to the PROTAC and to the antibody. 3. PROTAC(D).

PROTAC-Linker Conjugates for PAC Related Products (4):

Cat. No. Product Name CAS No. Purity Chemical Structure
  • HY-112100
    PROTAC ERα Degrader-5 2158322-33-7 98.96%
    PROTAC ERα Degrader-5 (compound LP2) consists an ADC linker and a PROTAC, whcih can be conjugated to an antibody to form PACs. PROTAC ERα Degrader-5 conjugated to an antibody is a more marked estrogen receptor-alpha (ERα) degrader compared to PROTAC (without Ab).
    PROTAC ERα Degrader-5
  • HY-133736
    PROTAC BRD4 Degrader-5-CO-PEG3-N3 2704602-92-4 99.73%
    PROTAC BRD4 Degrader-5-CO-PEG3-N3 (Compound 2) is a PROTAC-linker Conjugate for PAC, comprises the BRD4 degrader GNE-987 and PEG-based linker. PROTAC BRD4 Degrader-5-CO-PEG3-N3 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. Strain-promoted alkyne-azide cycloaddition (SPAAC) can also occur with molecules containing DBCO or BCN groups.
    PROTAC BRD4 Degrader-5-CO-PEG3-N3
  • HY-129938
    PROTAC BRD4 Degrader-24 2417370-39-7 99.61%
    PROTAC BRD4 Degrader-24 (compound 5), a PROTAC-linker Conjugate for PAC, comprises the chimeric BET degrader GNE-987 and disulfide-containing linker.
    PROTAC BRD4 Degrader-24
  • HY-160497
    MC-(β-Ala)-PABC-(β-D-GlcUA)-amide-PEG1-CH2-CC-885 2722697-86-9 99.63%
    MC-(β-Ala)-PABC-(β-D-GlcUA)-amide-PEG1-CH2-CC-885 (Comp Ie) is a neodegrader conjugate, can be used in the synthesis of antibody neoDegrader conjugate (AnDC).