PRN1371 is a highly selective and potent inhibitor of FGFR1-4 and CSF1R against FGFR1, FGFR2, FGFR3, FGFR4 and CSF1R IC50 The values are 0.6, 1.3, 4.1, 19.3, and 8.1 nM, respectively.
|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 Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 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 Compound A of 10 mg/kg.
|Solubility||DMSO ≥ 20 mg/mL|
 Ken A Brameld, et al. J Med Chem. Discovery of the Irreversible Covalent FGFR Inhibitor 8-(3-(4-Acryloylpiperazin-1-yl)propyl)-6-(2,6-dichloro-3,5-dimethoxyphenyl)-2-(methylamino)pyrido[2,3-d]pyrimidin-7(8H)-one (PRN1371) for the Treatment of Solid Tumors
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PF-05231023 is an FGF21-receptor agonist, it is also a potential treatment for T2DM.
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