FAK is a tyrosine kinase overexpressed in cancer cells and plays an important role in the progression of tumors to a malignant phenotype.
|PROTAC FAK degrader 1
|PROTAC FAK degrader 1 is a selective and potent PROTAC targeting on Fak with DC50 value of 3nM. It was generated by linking defactinib and VHL ligand.
|FC-11 is a potent FAK-targeting PROTAC. FC-11 showed a rapid and reversible FAK degradation with a picomolar of DC50 in various cell lines in vitro, which imply that FAK-PROTACs could be useful as expand tools for studying functions of FAK in biological system and as potential therapeutic agents.