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 Experiment | |
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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. |
Concentrations | 0~1µM |
Incubation time | 4 days |
Animal Experiment | |
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Animal models | H510 or H69 cells xenografts tumor bearing mice model |
Formulation | buffer alone |
Dosages | 50 mg/kg |
Administration | oral gavage |
Molecular Weight | 523.67 |
Formula | C28H41N7O3 |
CAS Number | 219580-11-7 |
Solubility (25°C) | DMSO 60 mg/mL |
Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
Species | Mouse | Rat | Rabbit | Guinea pig | Hamster | Dog |
Weight (kg) | 0.02 | 0.15 | 1.8 | 0.4 | 0.08 | 10 |
Body Surface Area (m2) | 0.007 | 0.025 | 0.15 | 0.05 | 0.02 | 0.5 |
Km factor | 3 | 6 | 12 | 8 | 5 | 20 |
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.
[3] Nicole J Chew, et al. FGFR3 signaling and function in triple negative breast cancer
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