CPL304110

CPL304110 is a potent, orally active and selective inhibitor of fibroblast growth factor receptors FGFR (1-3) , with IC 50 values of 0.75 nM, 0.5 nM, and 3.05 nM for FGFR (1-3), respectively In Vitro CPL304110 (0-0.6 μM) dose-dependently inhibits FGFR2 phosphorylation and downstream signaling (p-ERK). CPL304110 (compound 56q) exhibits in SNU-16 proliferation assay with an IC 50 of 85.64 nM. CPL304110 (compound 56q) demonstrats a more than 45-fold, 345-fold, 395-fold and 680-fold selectivity over KDR (VEGFR2), Flt3, Aura A and PDGFRb, respectively relative to FGFR2, and no significant inhibitory effects were observed with other tyrosine kinases. MCE has not independently confirmed the accuracy of these methods. They are for reference only. Western Blot AnalysisCell Line: SNU-16 cell lines. Concentration: 0-0.6 μM. Incubation Time: 1 h. Result: Suppressed FGFR2 phosphorylation and downstream signaling (p-ERK) In Vivo CPL304110 (p.o., 40 mg/kg) exhibits a t 1/2 of 2 h and C max of 3369 ng/mL in mice . CPL304110 (compound 56q, 2 X 20 mg/kg) significantly inhibits tumor growth in mice without significant body loss or any toxicity. On day 21 (D21, day of termination) the tumor growth inhibition (TGI) is 64% for dosing 20 mg/kg twice a day . MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: Severe combined immunodeficient (SCID) mice implanted subcutaneously with SNU-16 (human) . Dosage: 20 mg/kg (X2). Administration: Orally, twice daily for 21 days. Result: After 6 hours of last dosing, concentration of 56q decreased in the plasma (9%) but increased stepwise in the tumor cells (121%). IC50& Target:FGFR1 0.75 nM (IC 50 ) FGFR2 0.5 nM (IC 50 ) FGFR3 3.05 nM (IC 50 )

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