SSR128129E

SKU: orb1301089

Description

SSR128129E is an orally bioavailable, allosteric inhibitor that selectively targets FGFR1 with an IC50 of 1.9 μM. Its specificity makes it a valuable research tool for investigating FGFR1 signaling in cancer models, with applications in both in vitro biochemical assays and in vivo xenograft studies.

Research Area

Cardiovascular Research, Signal Transduction

Key Properties

• CAS Number: 848318-25-2
• MW: 346.31
• Purity: 99.87% (May vary between batches)
• Formula: C₁₈H₁₅N₂O₄·Na
• SMILES: [Na+].COc1c(C)c(C(=O)c2ccc(N)c(c2)C([O-])=O)n2ccccc12
• Target: FGFR
• Solubility: H2O:1 mg/mL (2.89 mM);Ethanol:< 1 mg/mL (insoluble or slightly soluble);10% DMSO+40% PEG300+5% Tween 80+45% Saline:2 mg/mL (5.78 mM);DMSO:45 mg/mL (129.94 mM)

Bioactivity

• Target IC50:
  FGFR1:1.9 μM
• 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. 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.
• 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.
• 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)

Storage & Handling

• Storage: Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

SSR, SSR 128129E, SSR128129E, SSR-128129E, FGFR, FGFR1

Compound Identifiers

PubChem CID

68853159