Fig. 3: Vepafestinib inhibits transmission of signals and blocks growth of cells with RET alterations. | Nature Cancer

Fig. 3: Vepafestinib inhibits transmission of signals and blocks growth of cells with RET alterations.

From: Vepafestinib is a pharmacologically advanced RET-selective inhibitor with high CNS penetration and inhibitory activity against RET solvent front mutations

Fig. 3

a, LUAD-0002AS1, ECLC5B and TT cells were serum starved for 24 h and then treated with the indicated concentrations of vepafestinib (TAS0953/HM06), selpercatinib, pralsetinib or vandetanib for 2 h. Following treatment, whole-cell extracts were prepared and subjected to western blotting analysis. Representative immunoblots from two independent experiments are shown. GAPDH was used as a loading control. RSK, ribosomal protein S6 kinase; S6RP, S6 ribosomal protein. b,c, Cells were plated in 96-well plates and treated for 96 h with the inhibitors shown. The number of viable cells was assessed using alamarBlue. b, Viability curves for control HBEC cells (HBECp53-EV) and HBEC cells with the CCDC6-RET fusion (HBECp53-RET) are shown at the left. Results are the mean ± s.e.m. of four independent experiments. Data were analyzed by non-linear regression, and IC50 values were estimated by curve fitting. A heatmap of the IC50 values is shown on the right. Missing values indicate that the experiment was not done. c, Viability curves for LUAD-0002AS1 (n = 3), ECLC5B (n = 3) and TT (n = 5) cells. Results are mean ± s.e.m. Each condition was assayed in triplicate for all viability studies.

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