FIIN 1 hydrochloride (Synonyms: FGFR irreversible inhibitor-1) |
| Catalog No.GC50051 |
FIIN 1 hydrochloride is a potent, irreversible, selective FGFR inhibitor. FIIN 1 hydrochloride binds to FGFR1/2/3/4 and Flt1/4 with Kds of 2.8/6.9/5.4/120 nM and 32/120 nM respectively. The biochemical IC50s of FIIN 1 hydrochloride are 9.2, 6.2, 11.9, and 189 nM against FGFR1/2/3/4, respectively.
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Cas No.: 1256152-35-8
Sample solution is provided at 25 µL, 10mM.
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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.
Zhou (2010) A structure-guided approach to creating covalent FGFR inhibitors. Chem.Biol. 17 285 PMID:20338520
Average Rating: 5 (Based on Reviews and 33 reference(s) in Google Scholar.)
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