CC-671 是一种双重 TTK 蛋白激酶/CLK2抑制剂, 对于 TTK 和 CLK2 的IC50值分别为 0.005 和 0.006 μM。

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

HCT-116 cell lysates treated with CC-671 at 3 μM for 1 h demonstrates that only four kinases show cellular binding of 75% or more including CLK2, CAMKK2, PIP4K22, and JNK[1].

CC-671 demonstrates significant tumor growth inhibition ((vehicle -treated/vehicle) ×100%) of 71% at both 10 and 20 mg/kg on a every 3 days (q3d) dosing schedule. The body weight loss in the CC-671 treated group (20 mg/kg ) is higher than in the 10 mg/kg group (17% vs 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].

1618658-88-0

C28H28N6O4

512.57

CC-671

DMSO:60 mg/mL
Powder: -20°C for 3 years
In solvent: -80°C for 2 years