BLU9931 Chemical Properties

Density 

1.361±0.06 g/cm3(Predicted)

storage temp. 

Store at -20°C

solubility 

≥50.9 mg/mL in DMSO; insoluble in H2O; ≥2.53 mg/mL in EtOH with gentle warming and ultrasonic

form 

Powder

pka

13.15±0.70(Predicted)

color 

Off-white to light yellow

BLU9931 Usage And Synthesis

Definition

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].

References

[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).

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