Athymic nu/nu female mice (Charles River Laboratories) were injected s.c. with either 5x10^6 A431. Mice were treated either i.p. or p.o. with a suspension of CL-387,785 prepared in 0.2% Klucel. Tumor growth inhibition was observed at doses 20-80 mg/kg ip, 80 mg/kg po.

Kinase assays were performed with a recombinant cytoplasmic domain of EGF-R. Stock solutions of 500 mM CL-387,785 (prepared in 100% DMSO) were diluted to the desired concentration with 30 mM HEPES, pH 7.4. Ten uL of CL-387,785 at various concentrations were incubated with 3 mL of recombinant enzyme on ice for 10 min. Then, 5 mL peptide, 10 mL of 43 reaction buffer, 0.30 mL [33P]ATP were added. After incubation for 90 min at room temperature, the entire volume was spotted onto precut P81 filter papers. The filter discs were washed two times with 0.5% phosphoric acid, and radioactivity was measured using a liquid scintillation counter. IC50 in this assay was 0.37 nM.