BLU9931

BLU9931 is a potent, highly selective, and irreversible fibroblast growth factor receptor 4 (FGFR4) inhibitor with an IC50 of 3 nM and a Kd of 6 nM. BLU9931 has significant antitumor activity. BLU9931 makes a covalent bond with Cys552 within the ATP-binding pocket of FGFR4, which is not present in FGFR1-3. BLU9931 inhibited gastric cancer cell growth in a transplanted mouse model[1].

[1] Norihiko Sasaki. “FGFR4 Inhibitor BLU9931 Attenuates Pancreatic Cancer Cell Proliferation and Invasion While Inducing Senescence: Evidence for Senolytic Therapy Potential in Pancreatic Cancer.” Cancers (2020).