FAK PROTAC B5

FAK PROTAC B5 (Compound B5) is a FAK PROTAC degrader with an IC50 value of 14.9 nM. FAK PROTAC B5 presents strong FAK degradation activity, antiproliferative activity, outstanding plasma stability and moderate membrane permeability. FAK PROTAC B5 inhibits cell migration and invasion[1].

Research Areas >> Cancer

Signaling Pathways >> Protein Tyrosine Kinase/RTK >> FAK

Signaling Pathways >> PROTAC >> PROTAC

IC50: 14.9 nM (FAK)[1]

FAK PROTAC B5 (Compound B5) displays strong antiproliferative activity (IC50 = 0.14 ± 0.01 μM) against A549 cells[1]. FAK PROTAC B5 displays excellent FAK degradation activity (86.4% at 10 nM) and the degradation is realized through proteasome degradation pathway[1]. FAK PROTAC B5 (0-1.8 μM, 72 h) has the significant ability to inhibit the migration of A549 cells[1]. FAK PROTAC B5 (0-1.8 μM, 72 h) inhibits the invasion of A549 cells in a concentration-dependent manner[1]. FAK PROTAC B5 exhibits a moderate membrane permeability[1]. Western Blot Analysis[1] Cell Line: A549 Concentration: 0.01 μM, 0.1 μM, 1 μM Incubation Time: 8 h Result: Reduced the level of FAK protein in a dose-dependent manner. Displayed excellent FAK degradation activity (86.4% at 10 nM). Cell Invasion Assay[1] Cell Line: A549 Concentration: 0.20, 0.60 and 1.80 μM Incubation Time: 72 h Result: Significantly reduced the number of A549 cells in a concentration-dependent manner.

FAK PROTAC B5 (Compound B5) possesses favorable plasma stability with the half-life value greater than 289.1 min[1].

[1]. Yin Sun, et al. Identification of novel and potent PROTACs targeting FAK for non-small cell lung cancer: Design, synthesis, and biological study. Eur J Med Chem. 2022 Apr 23;237:114373.