PROTAC FGFR2 degrader 2

PROTAC FGFR2 degrader 2 (compound 28E) (0.01-100 nM; 72 h) potently inhibits proliferation of FGFR2-overexpressing/amplified KATO III, SNU16, and AN3CA cells in vitro with IC₅₀ values of 0.794 nM, 0.207 nM, and 4.626 nM, respectively^[1].
PROTAC FGFR2 degrader 2 (72 h) potently inhibits proliferation of Ba/F3 ETV6-FGFR2 and Ba/F3 ETV6-FGFR3 cells with IC₅₀ values of 0.91 nM and 0.20 nM, respectively, while showing weaker activity against Ba/F3 ETV6-FGFR1 and Ba/F3 ETV6-FGFR4 cells^[1].
PROTAC FGFR2 degrader 2 (0.00508-1000 nM; 3-96 h) time- and concentration-dependently degrades FGFR2 protein in KATO III cells, with a DC₅₀ of 0.645 nM after 24 h treatment^[1].
PROTAC FGFR2 degrader 2 (0.411-300 nM; 24 h) exhibits highly selective degradation of FGFR2, with minimal to no degradation of FGFR1, FGFR3, FGFR4, or VEGFR2 in vitro^[1].
PROTAC FGFR2 degrader 2 (50 nM) mediates FGFR2 degradation in KATO III cells via the ubiquitin-proteasome pathway in a CRBN-dependent manner^[1].
PROTAC FGFR2 degrader 2 (0.1-10 nM; 24 h) inhibits FGFR2 downstream signaling (phosphorylation of FGFR2, PLCγ, and FRS2) in KATO III cells, with activity superior to LY2874455 (HY-13304) at equivalent concentrations^[1].
PROTAC FGFR2 degrader 2 potently inhibits FGFR2 kinase activity (IC₅₀ = 0.449 nM) and shows enhanced activity against the FGFR2^V564F gatekeeper mutant (IC₅₀ = 0.121 nM), with lower activity against FGFR4 compared to other FGFR isoforms^[1].
PROTAC FGFR2 degrader 2 (10 nM; 48 h) strongly inhibits migration of FGFR2-overexpressing AN3CA cells, with activity comparable to 100 nM LY2874455^[1].

PROTAC FGFR2 degrader 2 (0.1-10 nM; 24 h) induces G0/G1 phase cell cycle arrest in KATO III cells at concentrations as low as 0.1 nM, and downregulates cell cycle-associated proteins Cyclin D1, CDK4, and CDK6^[1].