Figure 1. Selectivity of MRTX1133 in Ras mutant human cancer cell lines.
A-C. Human cancer cell lines harboring KRAS or BRAF mutations were treated with MRTX1133 for 3 days. Cell viability was determined using the CellTiter-Glo assay. IC50 values was estimated from curve fitting using three independent repeats (error bars represent S.D. of 3 independent experiments; n.d., not determined). Arrow indicates concentration of MRTX1133 (10 μM) that causes non-specific toxicity.
D. Human cancer cell lines harboring KRAS or BRAF mutations were treated with 1 μM MRTX1133 (+) or DMSO (−) for one day. Cell lysates were harvested and immunoblotted for pERK and total ERK. Changes in the level of pERK relative to untreated sample was quantified and shown under the pERK blots (a representative of two independent experiments is shown).
E. INA-6 cells were treated with MRTX1133 or Trametinib for 3 days. Cell viability assay was performed analogously to that in panel A (error bars represent S.D. of 3 independent experiments).
F. INA-6 cells were treated with different concentrations of MRTX1133 or trametinib for one day. Cell lysates were harvested and immunoblotted for pERK and total ERK (a representative of two independent experiments is shown).