PD173074 is a potent and selective, ATP-competitive FGFR1 and FGFR3 inhibitor with IC50 values of 5, 21.5, ~100, 17600 and 19800 nM for FGFR3, FGFR1, VEGFR2, PDGFR and c-Src respectively. FGF receptor (FGFR) inhibitors exert their effects by activating cell surface receptor tyrosine kinases. PD173074 blocks H-510 and H-69 SCLC proliferation and clonogenic growth in a dose-dependent fashion and prevents FGF-2-induced chemoresistance. FGFR1 inhibitor PD 173074 potently and selectively antagonized the neurotrophic and neurotropic actions of FGF-2. PD 173074 displayed 1,000-fold differential IC(50) values for inhibition of FGF-2-stimulated neurite outgrowth in PC12 cells and in granule neurons, and FGF-2-induced mitogen-activated protein kinase (p44/42) phosphorylation. More dramatically, in H-69 xenografts, PD173074 induced complete responses lasting >6 months in 50% of mice.
|Cell lines||H510 and H69 cell lines|
|Preparation method||Cell proliferation assay H510 and H69 (1.5 × 104 cells/mL) in SITA were treated with or without FGF-2; PD173074 for the duration and at the concentration highlighted in the figure legends. Cell number was determined by cell counting.|
|Incubation time||4 days|
|Animal models||H510 or H69 cells xenografts tumor bearing mice model|
|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||DMSO ≥100 mg/mL
Ethanol ≥100 mg/mL
|Source||J Cardiovasc Pharmacol (2015). Figure 5.PD173074|
|Incubation Time||1 h|
|Results||Compared with the vehicle group, the ratio of phosphorylated ERK1/2 to total ERK1/2 was significantly decreased after PD173074 treatment.|
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