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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 | ¥ 1,220 | 5日内发货 | |
| 10 mg | ¥ 1,790 | 6-8周 | |
| 25 mg | ¥ 2,970 | 6-8周 | |
| 50 mg | ¥ 4,490 | 6-8周 | |
| 100 mg | ¥ 6,430 | 6-8周 | |
| 1 mL x 10 mM (in DMSO) | ¥ 1,130 | 6-8周 |
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| 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 |
| Smiles | CN(C)c1ccc(CC(=O)Nc2cc([nH]n2)C2CCC2)cc1 |
| 存储 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year Shipping with blue ice/Shipping at ambient temperature. 实际储存温度请以COA为准 |
对于不同动物的给药剂量换算,您也可以参考 更多