| Name | SSR128129E |
| Description | SSR128129E (SSR) is an allosteric and orally-active FGFR1 inhibitor (IC50: 1.9 μM), but not affecting other related RTKs. |
| Cell Research | 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, cell proliferation is assessed with the use of the CellTiter 96 AQueous One Solution Cell Proliferation Assay according to manufacturer’s instructions. 10 % FBS containing medium is used a positive control. (Only for Reference) |
| Kinase Assay | Scintillation Proximity Assay, 125I-FGF-2 Binding: SPA protein A beads are supplied as a suspension in PBS at 20 mg/mL, then diluted with binding buffer (KCl, 400 mg/L; MgSO4 200 mg/L; NaCl 6.4 g/L; NaHCO3 3.7 g/L; NaH2PO4 0.141 mg/mL; bis Tris Propane 11.292 g/L; Glucose 4.5 g/L; Gelatin 0.1 %; pH 7.0) at 10 mg/mL. 125I-FGF-2 radioligand and FGFR-1IIIc? - Fc Chimera are diluted into binding buffer. Binding was performed on 96-well plates coated with 0.1 % gelatin. Total assay volume is 0.1 mL. Binding of 125I-FGF-2 is determined by incubation of SPA beads coated with protein A (0.5 mg/assay) with FGFR-1IIIc? - Fc chimera soluble receptor (5 ng/assay), FGF-2 (20 ng/assay) is used for non-specific binding determinations. |
| In vitro | SSR128129E inhibited FGF2-induced EC proliferation and migration (IC50 =31 nM) and dose-dependently induced cilia formation.SSR128129E inhibited responses mediated by FGFR1-4. For example, SSR128129E blocks the migratory response of cardiomyocytes to FGF1 (ligand for FGFR1 and FGFR4) and the capillary formation response to FGF19 (ligand for FGFR4).
SSR128129E inhibited FGF7-induced proliferation and migration of the murine pancreatic Panc02 tumor cell line, suggesting that SSR128129E also inhibits FGFR isoforms in other species.[1] |
| In vivo | Oral administration of SSR128129E 30 mg/kg/day inhibited the growth of orthotopic Panc02 tumors by 44% starting on day 3 and delayed the growth of Lewis lung cancer. Tumor size and weight were reduced by 53% and 40%, respectively, starting on day 5.[1]
SSR128129E inhibited the growth of subcutaneous CT26 colon tumors and inhibited the growth of a multidrug-resistant MCF7/ADR breast cancer xenograft model.SSR128129E reduced the invasiveness of Panc02 tumor cells and metastasis to peritoneal lymph nodes.[1] |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
| Solubility Information | Ethanol : < 1 mg/mL (insoluble or slightly soluble)
H2O : 1 mg/mL (2.88 mM)
DMSO : 45 mg/mL (129.94 mM), Sonication is recommended.
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| Keywords | SSR-128129E | Fibroblast growth factor receptor | Inhibitor | SSR128129E | inhibit | FGFR |
| Inhibitors Related | Amlexanox | Nintedanib | Pazopanib Hydrochloride | Ferulic Acid | Nintedanib esylate | Ponatinib | Pemigatinib | Formononetin | Lenvatinib mesylate | Erdafitinib | Lenvatinib | Pazopanib |
| Related Compound Libraries | Highly Selective Inhibitor Library | Reprogramming Compound Library | Target-Focused Phenotypic Screening Library | Bioactive Compound Library | Membrane Protein-targeted Compound Library | Kinase Inhibitor Library | Tyrosine Kinase Inhibitor Library | Inhibitor Library | Bioactive Compounds Library Max | Anti-Cancer Compound Library |
United States
