SU5402 - CAS 215543-92-3 - Calbiochem (C15-1223-416)

General description

A cell-permeable, reversible, and ATP-competitive inhibitor of the tyrosine kinase activity of FGFR1 (IC₅₀ = 10-20 µM in the presence of 1 mM ATP) by interacting with the catalytic domain of FGFR1. Also inhibits aFGF-induced phosphorylation of ERK1 and ERK2 (IC₅₀ = 10-20 µM). In contrast to SU4984, it acts only as a weak inhibitor of tyrosine phosphorylation of the PDGF receptor. Does not inhibit the phosphorylation of insulin receptor and exhibits no inhibitory effect on EGF receptor kinase.

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.

Biochem/physiol Actions

Cell permeable: yes

Primary Target
Fibroblast growth factor receptor 1 (FGFR1)

Product competes with ATP.

Reversible: yes

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

Warning

Toxicity: Standard Handling (A)

Reconstitution

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.

Other Notes

Mohammadi, M., et al. 1997. Science 276, 955.

Legal Information

Not available for sale in the United States.

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany