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 相关产品 (3):

Cat. No. Product Name CAS No. Purity Chemical Structure
  • HY-112100
    PAC 2158322-33-7 98.17%
    PAC 由 ADC linker 和 PROTAC 分子组成,PAC 与抗体偶联。PAC 的详细信息请参考专利文献 WO2017201449A1 中的化合物 LP2。与 PROTAC (不偶联 Ab) 相比,PAC 偶联抗体之后更加显著降低雌激素受体-α (ERα) 水平。
  • HY-129938
    PROTAC BRD4 degrader for PAC-1 99.23%
    PROTAC BRD4 degrader for PAC-1 (compound 5),是一种用于 PAC 的 PROTAC- linker 偶联物,包含嵌合体 BET 降解剂 GNE-987 和含二硫化物的 linker。
    PROTAC BRD4 degrader for PAC-1
  • HY-133736
    PROTAC BRD4 Degrader-5-CO-PEG3-N3 99.54%
    PROTAC BRD4 Degrader-5-CO-PEG3-N3 (Compound 2) 一种用于 PAC 的 PROTAC- linker 偶联物,包含 BRD4 降解剂 GNE-987 和 3 个 PEG 的 linker。
    PROTAC BRD4 Degrader-5-CO-PEG3-N3