A. Osimertinib, compound-14, and combination (titrated
osimertinib + 1μM of Compound-14) dose-response curves for YU-005C cells.
B. Osimertinib, FHD-286, and combination (titrated osimertinib
+ 100nM of FHD-286) dose-response curves for YU-005C cells. (A,B) N=4. The mean
± standard deviation is shown. C. Bar graph of IC50 values
for YU-005C cells treated with osimertinib (alone), or in combination with
compound-14 or FHD-286. The mean ± SEM is shown. Significance was
calculated using the one-way repeated measures ANOVA test and Tukey’s
multiple comparisons test. ***P<0.001, **P<0.01, *P<0.05.
D. Experimental design. YU-005C cells were injected
subcutaneously in mice that were treated with either vehicle, osimertinib,
FHD-286 or the combination of both. E. Normalized tumor volume of
YU-005C cells treated with either vehicle, osimertinib, FHD-286 or the
combination. Individual tumor volumes reflect the change in volume from
treatment baseline. Tumor volume mean and ± standard error of the mean is
shown. Significance was calculated using the two-way repeated measures ANOVA
test and Dunnett’s multiple comparisons test, with a single pooled
variance. ***P<0.001, **P<0.01, *P<0.05. G.
Schematic representation of the mechanistic model by which SMARCA4 promotes
osimertinib resistance. Sensitive tumors rely on EGFR signaling pathway.
Osimertinib blocks EGFR and generates ROS killing the cells. Resistant tumors
rely on SMARCA4 to keep proliferating and neutralizing the accumulated ROS.
Blocking SMARCA4 activity generates stress killing the cells. Created with
Biorender.com. See also Figure
S7.