FIIN 1 hydrochloride

Catalog # Availability Size / Price Qty
4002/2
FIIN 1 hydrochloride | CAS No. 1256152-35-8 | FGF Receptor Inhibitors
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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%

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Biological Activity

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

M.Wt:
693.06
Formula:
C32H39Cl2N7O4
Solubility:
Soluble to 100 mM in DMSO and to 100 mM in ethanol
Purity:
≥96%
Storage:
Store at -20°C
CAS No:
1256152-35-8

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.

Background References

  1. A structure-guided approach to creating covalent FGFR inhibitors.
    Zhou
    Chem.Biol., 2010;17:285

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