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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 Biosci. 2025 Jan 17;15(1):4.
Human epicardial organoids from pluripotent stem cells resemble fetal stage with potential cardiomyocyte- transdifferentiation
PD173074 purchased from AbMole
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Source | J Cardiovasc Pharmacol (2015). Figure 5.PD173074 |
| Method | Western Blot | |
| Cell Lines | B-cell | |
| Concentrations | ||
| 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. |
| Cell Experiment | |
|---|---|
| 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 | |
|---|---|
| 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 |
[3] Nicole J Chew, et al. FGFR3 signaling and function in triple negative breast cancer
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