Table 2.

Structurally diverse selective Src inhibitors inhibit proliferation of human tumor cells grown under low serum conditions

Cells were plated at a density of 7,500 cells/well (HT-29) or 12,000 cells/well (MDA-MB-468 cells) in 96-well plates on day 0. Compounds were added on day 1, and the cells were incubated at 37°C for 2 days. Total cellular protein content was determined by staining cells with sulforhodamine B, and IC50 and LD50 values were calculated. IC50 indicates the inhibitor concentration required to reduce total protein accumulation by 50% relative to untreated cells; LD50 indicates the inhibitor concentration required to reduce total cellular protein by 50% relative to the starting amount (23). Similar values were obtained in two independent studies.

CompoundsHT-29
MDA-MB-468
Low serum
High serum
Low serum
High serum
IC50m)LD50m)IC50m)LD50m)IC50m)LD50m)IC50m)LD50m)
SU113330.83.96.912.01.64.54.09.0
SU113361.22.77.217.01.27.26.510.5
SU124700.85.56.812.01.57.84.59.5
CGP776750.85.05.021.00.38.03.016.0