Tos-PEG4-t-butyl ester (Tos-PEG4-Boc) 是一种 PROTAC 连接桥 (PROTAC linker)，属于 PEG 类。Tos-PEG4-t-butyl ester (Tos-PEG4-Boc) 可用于合成一系列 PROTAC 分子，如 BI-3663 。BI-3663 是一种高度选择性的 PTK2/FAK PROTAC，具有 E3 连接酶配体，能够降解 PTK2，IC50 值为 18 nM。
Tos-PEG4-t-butyl ester (Tos-PEG4-Boc) is a PROTAC linker, which refers to the PEG composition. Tos-PEG4-t-butyl ester (Tos-PEG4-Boc) can be used in the synthesis of a series of PROTACs, such as BI-3663 . BI-3663 is a highly selective PTK2/FAK PROTAC, with cereblon ligands to hijack E3 ligases for PTK2 degradation, and inhibits PTK2 with an IC50 of 18 nM[1].
[1]. Popow J, et al. Highly Selective PTK2 Proteolysis Targeting Chimeras to Probe Focal Adhesion Kinase Scaffolding Functions. J Med Chem. 2019 Mar 14;62(5):2508-2520.
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