RK-287107

一种TNKS1和TNKS2抑制剂（IC50值分别为0.014µM和0.010µM）；与PARP1、PARP2和PARP10相比，对TNKS1和TNKS2具有选择性（对PARP1、PARP2和PARP10的IC50值分别为>20µM、2.7µM和19.8µM）；在报告基因实验中抑制Wnt依赖性信号传导（IC50=0.077µM）；在COLO 320DM细胞中，以0.1µM浓度增加Axin2的积累；在COLO 320DM细胞中抑制细胞生长（GI50=0.45µM）；在COLO 320DM小鼠异种移植模型中，以150mg/kg剂量给药可减少肿瘤生长。A TNKS1 and TNKS2 inhibitor (IC50s = 0.014 and 0.010 µM, respectively); selective for TNKS1 and TNKS2 over PARP1, PARP2, and PARP10 (IC50s = >20, 2.7, and 19.8 µM, respectively); inhibits Wnt-dependent signaling (IC50 = 0.077 µM in a reporter assay); increases Axin2 accumulation in COLO 320DM cells at 0.1 µM; inhibits cell growth in COLO 320DM cells (GI50 = 0.45 µM); reduces tumor growth in a COLO 320DM mouse xenograft model at 150 mg/kg.分子式C22H26F2N4O2分子量416.5O=C1N=C(NC2=C1CCCC2)N3CCC4(C(C(F)=CC(F)=C5)=C5N(CCO)C4)CC3