Supplementary Table S1 and Supplementary Figures S1-S4 from Concomitant Inhibition of PI3Kβ and BRAF or MEK in PTEN-Deficient/<i>BRAF</i>-Mutant Melanoma Treatment: Preclinical Assessment of SAR260301 Oral PI3K<b>β</b>-Selective Inhibitor

Abstract

&lt;p&gt;Supplementary Tables S1. Table S1 describes the inhibitory activity of SAR260301 on AKT phosphorylation (Ser473 and Thr308) in a panel of tumor cell lines with different genetic abnormalities that are reported. Supplementary Figures S1-S4. Figure S1 illustrates the selectivity of SAR260301 against VPS34 in cellular setting: Figure S1A describes the activity of SAR260301 on VPS34 kinase function in GFP-FYVE cellular assay; Figure S1B describes the activity of SAR260301 on autophagy in GFP-LC3 cellular assays. Figure S2 describes the inhibitory activity of SAR260301 on the phosphorylation of AKT downstream effectors PRAS40 and S6RP in PC3 cell line, as a function of time. Figure S3 describes the in vitro antitumor activity of SAR260301: Figure S3A describes the antiproliferative activity of SAR260301on MEF-3T3-myr p110β cells. Figure S3B describes the antiproliferative activity of SAR260301on PC3 cells. Figure S3C describes the activity of SAR260301on PC3 cell death. Figure S3D describes the activity of SAR260301on LnCaP cell apoptosis. Figure S4 is a scheme describing the rationale for combining inhibitors of PI3K� and MAPK.&lt;/p&gt;