Fig. 7: Pharmacodynamic effects of CYpHER.
From: CYpHER: catalytic extracellular targeted protein degradation with high potency and durable effect
a Designs of various EGFR CYpHERs and control molecules. b and c A549 cells (unsorted, thus including live and dead cells) treated for 24 h with PBS, 10 nM CYpHER, or 10 nM control molecule followed by no treatment (“–”, EGFR, Actin) or addition of 50 ng/mL EGF for 30 min (“+”) and analyzed by Western blot for pY1068 EGFR (“–” and “+”), total EGFR, or actin. Full blots in Supplementary Figs. 14 and 15. d–h 96 well plate growth for 4 days (A431) or 7 days (all others) with single dose (no media exchange) of CT-1212-1, cetuximab, gefitinib, or osimertinib in A431 (d), H1975 (e), H1650 (f), A549 (g), and H358 (h) cells. After treatment, cell levels per well were quantitated by CellTiter-Glo 2.0 [CTG] assay. N = 3 wells per condition. See panel i for EC50 values and P values vs CT-1212-1; see Supplementary Data for details on statistical analysis. i EC50 values of the experiments in d–h from asymmetric sigmoidal (5PL) curve fit. Empty “X” box indicates no effect, as defined by failure to suppress growth by 20% at any dose tested. Experiments in b–h were conducted once (b, c, h) or twice (d–g) with similar results. See the Supplementary Data for full statistical breakdown. Source data are provided as a Source Data file.
