IC261 (20.5 mg/kg) inhibits tumor growth of PancTu-2 cells in SCID mice, downregulates several anti-apoptotic proteins, such as CK1δ/?, KRAS, and IL6 and upregulates p21, ATM, CHEK1 and STAT1 in mice
參考文獻(xiàn):
1. Mashhoon N, et al. Crystal structure of a conformation-selective casein kinase-1 inhibitor. J Biol Chem. 2000 Jun 30;275(26):20052-60. 2. St?ter M, et al. Inhibition of casein kinase I delta alters mitotic spindle formation and induces apoptosis in trophoblast cells. Oncogene. 2005 Dec 1;24(54):7964-75. 3. Brockschmidt C, et al. Anti-apoptotic and growth-stimulatory functions of CK1 delta and epsilon in ductal adenocarcinoma of the pancreas are inhibited by IC261 in vitro and in vivo. Gut. 2008 Jun;57(6):799-806