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CP681301 是CDK5的有效抑制剂,具有抗增殖活性。CP681301 在果蝇中表现出抗肿瘤活性。CP681301 降低神经胶质瘤干细胞中 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 是CDK5的有效抑制剂,具有抗增殖活性。CP681301 在果蝇中表现出抗肿瘤活性。CP681301 降低神经胶质瘤干细胞中 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。
规格 | 价格 | 库存 | 数量 |
---|---|---|---|
2 mg | ¥ 740 | 5日内发货 | |
5 mg | ¥ 1,230 | 5日内发货 | |
100 mg | ¥ 11,200 | 6-8周 |
产品描述 | CP681301 is a potent inhibitor of CDK5 with antiproliferative activity. CP681301 exhibits anti-tumor activity in Drosophila. CP681301 decreases the expression of CD133, OLIG2, SOX2, KI67, pCDK5 protein level in Glioma stem cells (GSCs). CP681301 reduces self-renewal in mouse glioma xenografts [1]. |
体外活性 | 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. |
体内活性 | 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. |
分子量 | 298.38 |
分子式 | C17H22N4O |
CAS No. | 865317-32-4 |
存储 | Shipping with blue ice. |
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