Biological Activity
Potent, irreversible FGFR inhibitor (Kd values are 2.8, 5.4, 6.9 and 120 nM for FGFR1, FGFR3, FGFR2 and FGFR4 respectively); acts at the ATP binding site. Also irreversibly inhibits Flt-1, Flt-4 and VEGFR-2 (Kd values are 32, 120 and 210 nM respectively); displays limited activity (Kd >500 nM) at other kinases. Exhibits antiproliferative activity in FGFR3- and FGFR1-transformed Ba/F3 cells (EC50 values are 10 and 14 nM respectively). Derived from the reversible FGFR inhibitor, PD 173074 (Cat. No. 3044).
Technical Data
| M. Wt | 693.06 |
| Formula | C32H39Cl2N7O4 |
| Storage | Store at -20°C |
| Purity | ≥96% (HPLC) |
| CAS Number | 1256152-35-8 |
| PubChem ID | 90488902 |
| InChI Key | IQLGDXNKTDKSMY-UHFFFAOYSA-N |
| Smiles | CCN(CC)CCCCNC1=NC=C2C(N(CC3=CC=CC(NC(C=C)=O)=C3)C(N(C4=C(Cl)C(OC)=CC(OC)=C4Cl)C2)=O)=N1.Cl |
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
All Tocris products are intended for laboratory research use only.
Solubility Data
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 69.31 | 100 | |
| ethanol | 69.31 | 100 |
Preparing Stock Solutions
The following data is based on the product molecular weight 693.06. Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 1.44 mL | 7.21 mL | 14.43 mL |
| 5 mM | 0.29 mL | 1.44 mL | 2.89 mL |
| 10 mM | 0.14 mL | 0.72 mL | 1.44 mL |
| 50 mM | 0.03 mL | 0.14 mL | 0.29 mL |
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Product Datasheets
References
References are publications that support the products' biological activity.
Zhou (2010) A structure-guided approach to creating covalent FGFR inhibitors. Chem.Biol. 17 285 PMID: 20338520
Keywords: FIIN 1 hydrochloride, supplier, FIIN1, hydrochloride, FGFR, fibroblast, growth, factors, receptors, irreversible, inhibits, inhibitors, PD173074, FGFR1, FGFR2, FGFR3, FGFR4, Flt-1, Flt-4, VEGFR2, FGFR, FGFR, Tocris Bioscience
