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• 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

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本计算器可帮助您计算出特定溶液中溶质的质量、溶液浓度和体积之间的关系，公式为：

质量 (mg) = 浓度 (mM) x 体积 (mL) x 分子摩尔量 (g/mol)

• pg ng μg mg g kg =
  fM pM nM μM mM M *
  nL μL mL L *