貨號(hào)	規(guī)格	價(jià)格	上海	北京	武漢	南京
S83824-2mg	99.6%	￥470.00 S83824-2mg ￥470.00 現(xiàn)貨	5 5	-	-	-
S83824-5mg	99.6%	￥860.00 S83824-5mg ￥860.00 現(xiàn)貨	6 6	-	-	-
S83824-10mg	99.6%	￥1700.00 S83824-10mg ￥1700.00 現(xiàn)貨	5 5	-	-	-
S83824-50mg	99.6%	￥5168.00 S83824-50mg ￥5168.00 現(xiàn)貨	2 2	-	-	-
S83824-100mg	≥98%	￥7900.00 S83824-100mg ￥7900.00 2-3天	0 貨期：2-3天	-	-	-

產(chǎn)品介紹

CCT251545 是一種有效的口服生物利用型的 WNT 信號(hào)抑制劑，在7dF3細(xì)胞中的IC50值為5 nM。CCT251545 還可作為選擇性化學(xué)探針，探討 CDK8 和 CDK19 在人類疾病中的作用

產(chǎn)品描述：

靶點(diǎn)：

CDK8; CDK19; Wnt(in 7dF3 cells):5 nM;Wnt/beta-catenin

體外研究：

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

體內(nèi)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

細(xì)胞實(shí)驗(yàn)：

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.

動(dòng)物實(shí)驗(yàn)：

Animal Models: Female NMRI mice, Male Wistar rats Dosages: 0.2 mg/kg, 0.5 mg/kg Administration: IV, Oral gavage

參考文獻(xiàn)：

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

保存條件：

-20℃

配置溶液濃度參考：

	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：

部分產(chǎn)品我司僅能提供部分信息，我司不保證所提供信息的權(quán)威性，僅供客戶參考交流研究之用。

參考文獻(xiàn)

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