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Submit ReviewFIIN 1 hydrochloride
Description: Potent, irreversible FGFR inhibitor
Chemical Name: N-(3-((3-(2,6-dichloro-3,5-dimethoxyphenyl)-7-(4-(diethylamino)butylamino)-2-oxo-3,4-dihydropyrimido[4,5-d]pyrimidin-1(2H)-yl)methyl)phenyl)acrylamide
Purity: ≥96% (HPLC)
Biological Activity for FIIN 1 hydrochloride
FIIN 1 hydrochloride is a 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 for FIIN 1 hydrochloride
| 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.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Solubility Data for FIIN 1 hydrochloride
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 69.31 | 100 | |
| ethanol | 69.31 | 100 |
Preparing Stock Solutions for FIIN 1 hydrochloride
The following data is based on the product molecular weight 693.06. Batch specific molecular weights may vary from batch to batch due to the degree 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 for FIIN 1 hydrochloride
References for FIIN 1 hydrochloride
References are publications that support the biological activity of the product.
Zhou (2010) A structure-guided approach to creating covalent FGFR inhibitors. Chem.Biol. 17 285 PMID: 20338520
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Keywords: FIIN 1 hydrochloride, FIIN 1 hydrochloride supplier, FIIN1, hydrochloride, FGFR, fibroblast, growth, factors, receptors, irreversible, inhibits, inhibitors, PD173074, FGFR1, FGFR2, FGFR3, FGFR4, Flt-1, Flt-4, VEGFR2, 4002, Tocris Bioscience
1 Citation for FIIN 1 hydrochloride
Citations are publications that use Tocris products. Selected citations for FIIN 1 hydrochloride include:
Ji Yeon et al (2013) Modulation of bevacizumab-induced toxicity for cultured human corneal fibroblasts. Invest Ophthalmol Vis Sci 54 3922-31 PMID: 23640039
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