SF2523

SF2523 is a dual inhibitor of phosphatidylinositol 3-kinase (PI3K; IC50 = 16 nM) and bromodomain-containing protein 4 (BRD4; IC50s = 241 and 1,550 nM for BRD4 bromodomains 1 and 2, respectively). It reduces MYCN gene expression, decreases MYCN and cyclin D1 protein levels, and inhibits phosphorylation of Akt in SKNBE2 cells. In vivo, SF2523 reduces tumor volume and protein levels of MYCN and cyclin D1 in a MYCN-amplified SKNBE2 neuroblastoma xenograft model in mice. It also reduces tumor growth and the number of colonic lymph node metastases in the murine orthotopic pancreatic Panc02 carcinoma...