CP681301
目录号 : GC68455CP681301 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。
Cas No.:865317-32-4
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
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. |
[1]. Mukherjee S, et al. CDK5 Inhibition Resolves PKA/cAMP-Independent Activation of CREB1 Signaling in Glioma Stem Cells. Cell Rep. 2018 May 8;23(6):1651-1664.
| Cas No. | 865317-32-4 | SDF | Download SDF |
| 分子式 | C17H22N4O | 分子量 | 298.38 |
| 溶解度 | DMSO : ≥ 100 mg/mL (335.14 mM) | 储存条件 | 4°C, protect from light |
| General tips | 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°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 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 |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。