CP681301 (C09-1119-607)

CP681301 is a potent CDK5 inhibitor. CP681301 shows antiproliferative activity. CP681301 decreases the expression of CD133 , OLIG2, SOX2, KI67, pCDK5 protein level in GSCs (Glioma stem cells). CP681301 reduces self-renewal in mouse glioma xenografts. CP681301 shows anti-tumor activity in Drosophila.In VitroCP681301 (1 µM; 96 h) shows variably cytotoxic to the tested GSC cultures but is not toxic to NHNPs. CP681301 (0, 10, 50 µM; 48 h) decreases the expression of CD133, OLIG2, SOX2, KI67, pCDK5 protein level in GSCs. CP681301 (0, 0.5, 1 µM; ) suppresses the expression of CREB Ser133 phosphorylation. MCE has not independently confirmed the accuracy of these methods. They are for reference only. Cell Cytotoxicity AssayCell Line: NHNP, N12.159, GBM121, GBM39, N08-74 cells Concentration: 1 µM Incubation Time: 96 h Result: Showed variably cytotoxic to the tested GSC cultures but was not toxic to NHNPs (normal human neuro-progenitors). Western Blot AnalysisCell Line: GBM 121, GBM39 cells Concentration: 1 µM Incubation Time: 48 h Result: Suppressed the expression of CD133, OLIG2, and SOX2 and cell proliferation marker KI67.In VivoCP681301 (1 mM; fed; 10 days) shows anti-tumor activity in 0- to 2-day-old adult Drosophila . MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: 0- to 2-day-old adult Drosophila (brat-RNAi tumors) Dosage: 1 mM Administration: Fed, 10 days Result: Reduced active phospho-dCdk5 (Y15) in tumor cells and the self-renewal properties of stem cells, increased the expression of neuronal marker ElaV in these cells and increased the median survival by 2.8-fold.Form:Solid. Specification: 0.99 Molecular Formula: C17H22N4O Molecular Weight: 298.38