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 Vitro CP681301 (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 Vivo CP681301 (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
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CP681301
CAS number：865317-32-4 molecular formula：C17H22N4O
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| Chinese alias | - | ||
| English alias | - | ||
| CAS number | 865317-32-4 | molecular formula | C17H22N4O |
| molecular weight | 298.38 g/mol | Exact mass | ≥99% |
| PSA | - | logp | - |
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