Erdafitinib (JNJ-42756493) is a potent and selective orally bioavailable, pan FGFR inhibitor with potential antineoplastic activity. Erdafitinib (JNJ-42756493) inhibits FGFR1/2/3/4 with IC50s of 1.2, 2.5, 3.0 and 5.7 nM, respectively.
In vivo, Erdafitinib administration results in potent and dose-dependent antitumor activity accompanied by pharmacodynamic modulation of phospho-FGFR and phospho-ERK in tumors.
|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 ≥ 40 mg/mL|
|Related FGFR Products|
EOC317 (ACTB-1003) is an orally available kinase inhibitor that inhibits FGFR1, VEGFR2, and tie-2 with IC50 values of 6,2, and 4 nM, respectively.
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.
Alofanib (RPT835) is a novel selective allosteric inhibitor of FGFR2 and has a dramatic inhibitory effect with IC50 <10 nM on FGF2-induced phoshphorylation of FRS2a in KATO III cells.
ASP5878 is a novel selective FGFR inhibitor with IC50 values of 0.47 nM, 0.6 nM, 0.74 nM and 3.5 nM for FGFR 1, 2, 3 and 4, respectively.
PF-05231023 is an FGF21-receptor agonist, it is also a potential treatment for T2DM.
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