A cell-permeable, reversible, and ATP-competitive inhibitor of the tyrosine kinase activity of fibroblast growth factor receptor 1 (FGFR1; IC50 = 10-20 µM in the presence of 1 mM ATP). Also inhibits aFGF-induced tyrosine phosphorylation of ERK1 and ERK2 (IC50 = 10-20 µM). In contrast to SU4984 (Cat. No. 572625), SU5402 is only a weak inhibitor of tyrosine phosphorylation of the PDGF receptor and does not inhibit phosphorylation of the insulin receptor. Does not inhibit the kinase activity of the EGF receptor. A 10 mM (500 µg/169 µl) solution of SU5402 (Cat. No. 572631) in DMSO is also available.
Synonyms: SU5402 - CAS 215543-92-3 - Calbiochem; 3-[3-(2-Carboxyethyl)-4-methylpyrrol-2-methylidenyl]-2-indolinone
Molecular Formula: C17H16N2O3
Molecular Weight: 296.32
Linear Structural Formula: C17H16N2O3
MDL Number: MFCD08235144
Purity: >=95% (HPLC)
Biochem Physiol Actions: Target IC50: 10-20 &10-20 µM for fibroblast growth factor receptor 1 (FGFR1) in the presence of 1 mM ATP;M against FGFR1 in the presence of 1 mM ATP; 10-20 µM against inhibits aFGF-induced tyrosine phosphorylation of ERK1 and ERK2
Legal Information: Not available for sale in the United States.
Other Notes: Mohammadi, M., et al. 1997. Science 276, 955.