CC-671 is a dual TTK protein kinase (IC50: 0.005 μM) /CLK2 (IC50: 0.006 μM) inhibitor.

TTK:0.005 μM, CLK2:0.006 μM

HCT-116细胞裂解物经3 μM的CC-671处理1小时后的结果表明，仅有四种激酶展示了75%或更高的细胞结合量，包括CLK2、CAMKK2、PIP4K22和JNK[1]。

CC-671在10mg/kg和20mg/kg剂量下，每3天给药一次的方案中显示出显著的肿瘤生长抑制效果，抑制率达71%（（vehicle-treated/vehicle）×100%）。在20mg/kg剂量的CC-671处理组中，体重损失比10mg/kg组更高（17%对比5%）[1]。

The kinase selectivity profile of CC-671 is assessed. The screen is conducted with the concentration of CC-671 held constant at 3 μM. The TTK binding affinity is measured using the kinase binding assays. The kinase binding assays are based on the binding and displacement of a proprietary, Alexa Fluor 647-labeled, ATP-competitive kinase inhibitor scaffold[1].

Female SCID mice are inoculated subcutaneously with 5×106 Cal-51 cells. Mice with tumours of approximately 125 mm3 are randomized and treated intravenously at various doses and schedules of CC-671 (n=8 to10/group). Tumours are measured twice a week for the duration of the study. The long and short axes of each a tumour are measured using a digital calliper in millimetres and the tumour volumes are calculated[1].