EGFR Inhibitor

Biochem/physiol Actions

Reversible: no

Product competes with ATP.

Target IC₅₀: 21 nM, 63 nM, and 4 nM for EGFRwt, EGFRL858R and EGFRL861Q, respectively

Cell permeable: yes

General description

A cell-permeable 4,6-dianilinopyrimidine compound that acts as a potent, ATP-competitive, and highly selective inhibitor of EGFR and some EGFR mutants (IC₅₀ = 21 nM, 63 nM, and 4 nM for EGFRwt, EGFR^L858R and EGFR^L861Q, respectively) vs. erbB4/Her4 (IC₅₀ = 7.64 µM) and a panel of 55 other kinases. Shown to completely block EGF-induced EGFR autophosphorylation in U-2OS cells at 10 µM.

Legal Information

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

Other Notes

Zhang, Q., et al. 2006. J. Am. Chem. Soc.128, 2182

Packaging

1 mg in Plastic ampoule

Packaged under inert gas

Warning

Toxicity: Standard Handling (A)