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。
Description | PAC comprises an antibody conjugated via a linker to a PROTAC. PAC extracts from patent WO2017201449A1, compound PAC1. PAC is a more marked estrogen receptor-alpha (ERα) degrader compared to PROTAC (without Ab). | ||||||||||||||||
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IC50 & Target | Estrogen receptor-alpha (ERα)[1] | ||||||||||||||||
In Vitro | Treatment of HER2 expressing cells with HER2 antibody containing PAC Anti-HER2(Endox-XIAP) results in a marked decreased Estrogen Receptor-alpha (ERα) levels with an IC50 of 132 ng/mL. 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 group (“E3LB”), a linker (“L2”) and a protein binding group (“PB”). The following sections describe the components that comprise the PAC. 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) [1]. | ||||||||||||||||
Solvent & Solubility | In Vitro: 10 mM in DMSO Preparing Stock Solutions
* Please refer to the solubility information to select the appropriate solvent. | ||||||||||||||||
References |
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