In vitro：BLU-554 exploits a unique interaction with FGFR4 to confer potency and selectivity. In vivo: BLU-554 is well tolerated in these tumor models. Administration of BLU-554 induces tumor regression in liver cancer models.
|Body Surface Area (m2)||0.007||0.025||0.15||0.05||0.02||0.5|
|Animal A (mg/kg) = Animal B (mg/kg) multiplied by||Animal B Km|
|Animal A Km|
For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.
|Solubility||100 mg/mL in DMSO|
First Selective Small Molecule Inhibitor of FGFR4 for the Treatment of Hepatocellular Carcinomas with an Activated FGFR4 Signaling Pathway.
Hagel M, et al. Cancer Discov. 2015 Apr;5(4):424-37. PMID: 25776529.
|Related FGFR Products|
FIIN-3 is a potent, selective, irreversible and the next-generation covalent FGFR inhibitor with IC50 values of 13.1, 21, 31.4 and 35.3 nM for FGFR1, FGFR2, FGFR3 and FGFR4, respectively.
FGFR4-IN-1 is a potent and selective FGFR4 inhibitor with IC50 of 0.7 nM.
FGF-401 is an inhibitor of FGFR4 extracted from patent WO2015059668A1, compound example 83; has an IC50 of 1.9 nM.
PD-166866 is a synthetic molecule inhibiting the tyrosin kinase action of FGFR1, shows a very high selectivity towards FGFR1 and inhibits the auto-phosphorylation activity of FGRF1.
BLU9931 is a potent, selective, and irreversible FGFR4 inhibitor with IC50 of 3 nM, about 297-, 184-, and 50-fold selectivity over FGFR1/2/3, respectively.
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