FIIN 1 hydrochloride (Synonyms: FGFR irreversible inhibitor-1) |
Catalog No.GC50051 |
El clorhidrato de FIIN 1 es un inhibidor de FGFR selectivo, irreversible y potente. El clorhidrato de FIIN 1 se une a FGFR1/2/3/4 y Flt1/4 con Kds de 2,8/6,9/5,4/120 nM y 32/120 nM respectivamente. Las CI50 bioquÍmicas del clorhidrato de FIIN 1 son 9,2, 6,2, 11,9 y 189 nM frente a FGFR1/2/3/4, respectivamente.
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Cas No.: 1256152-35-8
Sample solution is provided at 25 µL, 10mM.
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
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