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PROTAC-linker Conjugate for PAC

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).

Products for  PROTAC-linker Conjugate for PAC

  1. Cat.No. 产品名称 Information
  2. GC34151 PAC PAC是由抗体通过linker与PROTAC偶联而组成的。PAC的详细信息请参考专利文献WO2017201449A1中的化合物PAC1。与PROTAC(无Ab)相比,PAC更加显著降低雌激素受体-α(ERα)水平。
  3. GC61213 PROTAC BRD4 Degrader-5-CO-PEG3-N3 PROTACBRD4Degrader-5-CO-PEG3-N3(Compound2)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。

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