CP681301 是一种有效的CDK5抑制剂。CP681301 显示出抗增殖活性。CP681301 降低 GSC 中 CD133、OLIG2、SOX2、KI67、pCDK5 蛋白水平的表达。CP681301 减少小鼠胶质瘤异种移植物的自我更新。CP681301 在果蝇中显示出抗肿瘤活性。

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 [1].

CP681301 (1 μM; 96 h) shows variably cytotoxic to the tested GSC cultures but is not toxic to NHNPs [1]. CP681301 (0, 10, 50 μM; 48 h) decreases the expression of CD133, OLIG2, SOX2, KI67, pCDK5 protein level in GSCs [1]. CP681301 (0, 0.5, 1 μM; ) suppresses the expression of CREB Ser133 phosphorylation [1]. Cell Cytotoxicity Assay [1] Cell 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 Analysis [1] Cell 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.

CP681301 (1 mM; fed; 10 days) shows anti-tumor activity in 0- to 2-day-old adult Drosophila [1]. Animal Model: 0- to 2-day-old adult Drosophila (brat-RNAi tumors) [1] 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.

865317-32-4

C17H22N4O

298.38

(< 1 mg/ml refers to the product slightly soluble or insoluble )
Powder: -20°C for 3 years
In solvent: -80°C for 2 years