CPI-203 (RO-6870810, TEN-010, JQ2, and RG-6146)

Description: CPI-203 (RO6870810, JQ-2, TEN010, RG6146) is a novel, selective, cell permeable and orally bioavailable BET bromodomain inhibitor with anticancer activity. It inhibits BRD4 with an IC50 of 37 nM in a BRD4 alpha-screen assay. CPI 203 shows potent in vitro antiproliferative activity and high in vivo antitumor efficacy. CPI203 can enhance the antiproliferative effects of rapamycin on human neuroendocrine tumors. CPI203 can downregulate Myc expression, causes G1 cell cycle arrest and attenuate cell proliferation in human pancreatic neuroendocrine tumors. CPI203 arrests the growth of T cell acute lymphoblastic leukemia cells in vitro (EC50 = 91.2 nM).

References: Proc Natl Acad Sci U S A. 2012 May 1; 109(18):6927-32; Leukemia. 2014 Oct; 28(10):2049-59.