Potency assay (cells):
Average from three p53-positive cancer cell lines (SJSA1, RKO, and HCT116) in MTT assay. RG7388 was 344-fold more potent in this assay against p53-positive cells compared with p53-negative cells.
Target engagement assay (cells):
In SJSA1 cells, RG7388 led to dose-dependent accumulation of p53 and expression of p53-dependent genes (p21, MDM2).