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).
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.
A structure-guided approach to creating covalent FGFR inhibitors.