CCT245737, at a concentration of 10 µM, demonstrates significant inhibition (>80%) across a wide panel of 124 kinases, notably including ERK8, PKD1, RSK2, and RSK1, with IC50 values of 130, 298, 361, and 362 nM, respectively[1]. CCT245737 effectively disrupts the G2 checkpoint induced by VP-16 in various cell lines such as HT29, SW620, MiaPaCa-2, and Calu6, showcasing IC50 values ranging from 30 to 220 nM[2].
体内研究
When administered orally at 150 mg/kg, CCT245737 synergizes with LY 188011 (intravenously at 100 mg/kg) to inhibit tumor growth in HT29 colon cancer xenograft models. Furthermore, a dose of 300 mg/kg orally inhibits CHK1 autophosphorylation at Ser296 induced by LY 188011 (60 mg/kg intravenously) in SW620 colon cancer xenografts 24 hours post-treatment[1].
CCT245737, at 150 mg/kg orally, also markedly suppresses tumor growth in an Eμ-Myc mouse model of human B-cell lymphocytic leukemia[2].
体外研究
CCT245737, at a concentration of 10 µM, demonstrates significant inhibition (>80%) across a wide panel of 124 kinases, notably including ERK8, PKD1, RSK2, and RSK1, with IC50 values of 130, 298, 361, and 362 nM, respectively[1].
CCT245737 effectively disrupts the G2 checkpoint induced by VP-16 in various cell lines such as HT29, SW620, MiaPaCa-2, and Calu6, showcasing IC50 values ranging from 30 to 220 nM[2].
作用机制
CCT245737 binds in the ATP pocket of human CHK1. It is an ATP competitive inhibitor.
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