| 产品描述： | CCT251545 是一种有效的口服生物利用型的 WNT 信号抑制剂，在7dF3细胞中的IC50值为5 nM。CCT251545 还可作为选择性化学探针，探讨 CDK8 和 CDK19 在人类疾病中的作用 |
| 靶点： |
CDK8; CDK19; Wnt(in 7dF3 cells):5 nM;Wnt/beta-catenin |
| 体外研究： |
The suppression of the WNT pathway activity by CCT251545 is not unique to a specific cell line, is independent of exogenous WNT pathway stimulation, does not result from destabilization of TCF1 or TCF4, and is not due to interference with the luciferase-based reporter readout. CCT251545 also demonstrates a lack of transporter-mediated efflux and a lack of activity across broad in vitro panels of enzyme, receptor, and ion channel targets |
| 体内研究： |
CCT251545 is a potent small-molecule inhibitor of WNT signaling with good oral pharmacokinetics. We demonstrate inhibition of WNT pathway activity in a solid human tumor xenograft model with evidence for tumor growth inhibition following oral dosing |
| 细胞实验： |
Cell lines: 7dF3 cells, HEK293 cells, SW480, LS174T, COLO205 human colorectal cancer cells Concentrations: 9.1 μM - 0.068 nM Incubation Time: 2 h, 6 h Method: Taqman Assays. 7dF3 cells are seeded at 20 000 cells/well into 96-well cell culture plates. After overnight incubation the cells are treated with CCT251545 at concentrations ranging from 9.1 μM to 0.068 nM. After 2 or 6 h of incubation, cells are washed with PBS and stored at −80 ℃. Cells are lysed in Cells-to-cDNA II Cell lysis buffer and transferred to PCR plates. |
| 动物实验： |
Animal Models: Female NMRI mice, Male Wistar rats Dosages: 0.2 mg/kg, 0.5 mg/kg Administration: IV, Oral gavage |
| 参考文献： |
1. Aurélie Mallinger, et al. Discovery of potent, orally bioavailable, small-molecule inhibitors of WNT signaling from a cell-based pathway screen. J Med Chem. 2015 Feb 26;58(4):1717-35. 2. Trevor Dale, et al. A selective chemical probe for exploring the role of CDK8 and CDK19 in human disease. Nat Chem Biol. 2015 Dec;11(12):973-980. |
| 溶解性： |
Soluble in DMSO、Ethanol |
| 保存条件： |
-20℃ |
| 配置溶液浓度参考： |
|
1mg |
5mg |
10mg |
| 1 mM |
2.37 ml |
11.851 ml |
23.701 ml |
| 5 mM |
0.474 ml |
2.37 ml |
4.74 ml |
| 10 mM |
0.237 ml |
1.185 ml |
2.37 ml |
| 50 mM |
0.047 ml |
0.237 ml |
0.474 ml |
|
| 注意： |
部分产品我司仅能提供部分信息，我司不保证所提供信息的权威性，仅供客户参考交流研究之用。 |
上海工商
危险品化学品经营许可证（不带存储）
营业执照(三证合一)
北京