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. 2023 Jun 4;13(9):2012–2031. doi: 10.1158/2159-8290.CD-23-0475

Figure 2.

Figure 2. RLY-4008 inhibits FGFR2-mediated signaling and proliferation in cells. A, Inhibition of FGFR2-mediated signaling in SNU-16 cells. Cells were incubated with RLY-4008 for 2 hours prior to lysis and analysis via pFGFR2 (Y653/654) and pERK (T202/Y204) HTRF (PerkinElmer). B, Inhibition of FGFR2-mediated signaling and induction of apoptosis in SNU-16 cells. Immunoblots of cell lysates generated from cells treated with DMSO (Control), IC50, or IC90 concentrations of RLY-4008 (as determined by pFGFR2 HTRF) for the indicated times. Samples were analyzed via traditional Western or via WES (Protein Simple). Loading controls were actin (traditional) and actin and vinculin (WES). cl, cleaved; p, phospho; t, total. C, Viability IC50 values for RLY-4008 in FGFR2-, FGFR1-, FGFR3-, and FGFR4-dependent cancer cell lines (Supplementary Table S3). Cells were treated for 96 hours and cellular viability was assayed using CellTiter-Glo (Promega). Average IC50 of two independent experiments each containing two biological replicates is reported. Error bars indicate SD. * Indicates that IC50 was not reached in this cell line (maximum RLY-4008 concentration = 10 μmol/L).

RLY-4008 inhibits FGFR2-mediated signaling and proliferation in cells. A, Inhibition of FGFR2-mediated signaling in SNU-16 cells. Cells were incubated with RLY-4008 for 2 hours prior to lysis and analysis via pFGFR2 (Y653/654) and pERK (T202/Y204) HTRF (PerkinElmer). B, Inhibition of FGFR2-mediated signaling and induction of apoptosis in SNU-16 cells. Immunoblots of cell lysates generated from cells treated with DMSO (Control), IC50, or IC90 concentrations of RLY-4008 (as determined by pFGFR2 HTRF) for the indicated times. Samples were analyzed via traditional Western or via WES (Protein Simple). Loading controls were actin (traditional) and actin and vinculin (WES). cl, cleaved; p, phospho; t, total. C, Viability IC50 values for RLY-4008 in FGFR2-, FGFR1-, FGFR3-, and FGFR4-dependent cancer cell lines (Supplementary Table S3). Cells were treated for 96 hours and cellular viability was assayed using CellTiter-Glo (Promega). Average IC50 of two independent experiments each containing two biological replicates is reported. Error bars indicate SD. * Indicates that IC50 was not reached in this cell line (maximum RLY-4008 concentration = 10 μmol/L).