FGFR1 Degrader

BR-cpd7 is an orally active, selective PROTAC degrader targeting FGFR1 and FGFR2, with a DC₅₀ of 2.2 nM against FGFR1. BR-cpd7 reduces FGFR signaling. BR-cpd7 induces cell cycle arrest and selectively blocks the proliferation of FGFR1/FGFR2-dependent tumor cells. BR-cpd7 exhibits significant antitumor efficacy in FGFR1-dependent lung cancer animal models, while achieving complete depletion of FGFR1. BR-cpd7 can be used for cancer-related research.

DGY-09-192 is a PROTAC FGFR1/2 degrader (FGFR1: DC₅₀ = 4.35 nM; FGFR2: DC₅₀ = 70 nM). DGY-09-192 preferentially degrades wild-type FGFR1/2 and multiple FGFR2 fusion proteins (including FGFR2-PHGDH and FGFR2-OPTN). DGY-09-192 suppresses downstream FGFR signaling (reducing phosphorylation of FRS2 Y196 and ERK1/2 T202/Y204) in vitro and vivo. DGY-09-192 can be used for the study of FGFR-driven cancers.

CYB-5067 is a FGFR molecular glue degrader with a DC₅₀ of 27 nM against FGFR2. CYB-5067 inhibits FGFR1, FGFR3, FGFR4 and downstream FGFR signaling pathways, induces antiproliferative activity in vitro, and exhibits sustained target protein inhibition in vivo without obvious hook effect. CYB-5067 shows significant tumor growth inhibitory activity in the ETV6-FGFR2 fusion Ba/F3 xenograft model. CYB-5067 can be used for the research of FGFR-driven cancers.