1400284-80-1
1400284-80-1 结构式
物理化学性质
沸点731.0±70.0 °C(Predicted)
密度1.34±0.1 g/cm3(Predicted)
储存条件-20°C储存
溶解度溶于二甲基亚砜
酸度系数(pKa)7.86±0.30(Predicted)
形态Solid
颜色Light yellow to brown
应用领域
用途一
CCT251455 is a potent and selecltive MSP1 inhibitor with potential anticancer activitiy. The protein kinase MPS1 is a crucial component of the spindle assembly checkpoint signal and is aberrantly overexpressed in many human cancers. MPS1 is one of the top 25 genes overexpressed in tumors with chromosomal instability and aneuploidy. PTEN-deficient breast tumor cells are particularly dependent upon MPS1 for their survival, making it a target of significant interest in oncology. CCT251455 stabilizes an inactive conformation of MPS1 with the activation loop ordered in a manner incompatible with ATP and substrate-peptide binding; it displays a favorable oral pharmacokinetic profile, shows dose-dependent inhibition of MPS1 in an HCT116 human tumor xenograft model, and is an attractive tool compound to elucidate further the therapeutic potential of MPS1 inhibition.