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SSR128129E is an orally-active and allosteric FGFR1 inhibitor with IC50 of 1.9 μM, while not affecting other related RTKs.
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Source | PLoS One (2013). Figure 3. SSR128129E |
| Method | qPCR | |
| Cell Lines | C57BL/6 | |
| Concentrations | 50 mg/kg/d | |
| Incubation Time | - | |
| Results | Treatment of apoE-deficient mice with SSR128129E did not affect the mRNA levels of all the receptors but FGFR2, the levels of which were slightly, but significantly, reduced |
| Cell Experiment | |
|---|---|
| Cell lines | Endothelial cells (ECs) and Panc02 tumor cells |
| Preparation method | Cell proliferation of porcine aortic endothelial (PAE) and tumor cell lines is analyzed on exponentially growing cells that are starved for 16 hours in 0.2 % FBS containing medium and seeded at 4,000 cells/well in 96-well microplates. After exposure to mitogens and/or SSR for 72 hours, according to manufacturer’s instructions, assessing the cell proliferation with the use of the CellTiter 96 AQueous One Solution Cell Proliferation Assay . 10 % FBS containing medium is used a positive control |
| Concentrations | ~100 nM |
| Incubation time | 72 hours |
| Animal Experiment | |
|---|---|
| Animal models | Mouse model of Arthritic and mouse tumor model bearing pancreatic tumor cell line Panc02, murine mammary carcinoma cell line 4T1, murine colon cancer cell line CT26, or human breast MCF7/ADR cell line. |
| Formulation | 0.6 % methylcellulose |
| Dosages | ~30 mg/kg |
| Administration | Oral administration |
| Molecular Weight | 346.31 |
| Formula | C18H15N2O4.Na |
| CAS Number | 848318-25-2 |
| Solubility (25°C) | DMSO 50 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
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