| References: |
CCT244747 inhibited cellular CHK1 activity (IC(50) 29-170 nmol/L), significantly enhanced the cytotoxicity of several anticancer drugs, and abrogated drug-induced S and G(2) arrest in multiple tumor cell lines. Biomarkers of CHK1 (pS296 CHK1) activity and cell-cycle inactivity (pY15 CDK1) were induced by genotoxics and inhibited by CCT244747 both in vitro and in vivo, producing enhanced DNA damage and apoptosis. Active tumor concentrations of CCT244747 were obtained following oral administration. The antitumor activity of both gemcitabine and irinotecan were significantly enhanced by CCT244747 in several human tumor xenografts, giving concomitant biomarker modulation indicative of CHK1 inhibition. CCT244747 also showed marked antitumor activity as a single agent in a MYCN-driven neuroblastoma. For the detailed information of CCT244747, the solubility of CCT244747 in water, the solubility of CCT244747 in DMSO, the solubility of CCT244747 in PBS buffer, the animal experiment (test) of CCT244747, the cell expriment (test) of CCT244747, the in vivo, in vitro and clinical trial test of CCT244747, the EC50, IC50,and affinity,of CCT244747, For the detailed information of CCT244747, the solubility of CCT244747 in water, the solubility of CCT244747 in DMSO, the solubility of CCT244747 in PBS buffer, the animal experiment (test) of CCT244747, the cell expriment (test) of CCT244747, the in vivo, in vitro and clinical trial test of CCT244747, the EC50, IC50,and affinity,of CCT244747, Please contact DC Chemicals. |
