PARP抑制剂;PARP Inhibitors;产品介绍:RK-287107 是一种新型有效且具有选择性及抗肿瘤活性的 tankyrase 的抑制剂。RK-287107 可抑制 tankyrase-1 和 tankyrase-2,在体外实验中其IC50值为14.3 nM和10.6 nM。;InformationRK-287107 RK-287107 is a novel, potent and selective tankyrase inhibitor with antitumor activity. RK-287107 inhibits tankyrase-1 and tankyrase-2 in vitro with IC50 of 14.3 nM and 10.6 nM.TargetsTankyrase-2 (Cell-free assay); Tankyrase-1 (Cell-free assay) 10.6 nM; 14.3 nMIn vitroRK-287107 is a novel tankyrase-specific inhibitor that inhibits tankyrase-1 and -2. RK-287107 causes Axin2 accumulation and downregulates β-catenin, T-cell factor/lymphoid enhancer factor reporter activity and the target gene expression in colorectal cancer cells harboring the shortly truncated APC mutations. Consistently, RK-287107 inhibits the growth of APC-mutated (β-catenin-dependent) colorectal cancer COLO-320DM and SW403 cells but not the APC-wild (β-catenin-independent) colorectal cancer RKO cells.In vivoIntraperitoneal or oral administration of RK-287107 suppresses COLO-320DM tumor growth in NOD-SCID mice. RK-287107 suppresses the Wnt/β-catenin pathway and tumor growth of the xenografted COLO-320DM cells in vivo.Cell Research(from reference)Cell lines:COLO-320DM, HCC2998, HCT-116, DLD-1, SW403, RKO Concentrations:0.01-10 μM Incubation Time:120 h