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。
| 生物活性 | CP681301 is a potentCDK5inhibitor. CP681301 shows antiproliferative activity. CP681301 decreases the expression ofCD133, OLIG2, SOX2, KI67, pCDK5 protein level in GSCs (Glioma stem cells). CP681301 reduces self-renewal in mouse glioma xenografts. CP681301 shows anti-tumor activity inDrosophila[1]. |
体外研究
(In Vitro) | 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. |
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体内研究
(In Vivo) | CP681301 (1 mM; fed; 10 days) shows anti-tumor activity in 0- to 2-day-old adultDrosophila[1].
| Animal Model: | 0- to 2-day-old adultDrosophila(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. |
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| 运输条件 | Room temperature in continental US; may vary elsewhere. |
| 储存方式 | 4°C, protect from light *In solvent : -80°C, 6 months; -20°C, 1 month (protect from light) |
| 溶解性数据 | In Vitro: DMSO : ≥ 100 mg/mL(335.14 mM) *"≥" means soluble, but saturation unknown. 配制储备液 | 1 mM | 3.3514 mL | 16.7572 mL | 33.5143 mL | | 5 mM | 0.6703 mL | 3.3514 mL | 6.7029 mL | | 10 mM | 0.3351 mL | 1.6757 mL | 3.3514 mL |
*请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80℃, 6 months; -20℃, 1 month (protect from light)。-80℃ 储存时，请在 6 个月内使用，-20℃ 储存时，请在 1 个月内使用。 |
