Fig. 4: Selective inhibition of oncogenic signalling and KRAS-driven tumour growth.
From: Pan-KRAS inhibitor disables oncogenic signalling and tumour growth
a, Thirty-nine cell lines were treated for 2 h to determine the effect on KRAS activation and downstream signalling. b, HEK293 cells expressing the indicated KRAS mutants were treated as shown and analysed to determine the effect on KRAS activation. The abundance (Pts) and distribution of mutations across cancer types (Cancer, %) are shown. c, A split luciferase assay was used to determine the rate constant for the inhibition of the KRAS–CRAF interaction by treatment in live cells (mean ± s.e.m., n = 3). d, Effect of KRASi treatment on the transcriptional output by key RAS effector pathways (median, interquartile range and Tukey whiskers). The number of effector-dependent genes used to calculate the output score is shown in parentheses. e, Profiling of IC50s in a panel of 274 cell lines. f, Mice bearing xenograft models were treated to determine the effect on tumour growth and animal weight (mean ± s.e.m., n = 5). FrC, fractional change (%).
