CCT251545

製品コードS7981 バッチS798101

化学情報

	Synonyms	N/A	Storage (From the date of receipt)	3 years -20°C powder
	化学式	C₂₃H₂₄ClN₅O
	分子量	421.92	CAS No.	1661839-45-7
Solubility (25°C)*	体外	DMSO	30 mg/mL (71.1 mM)
		Ethanol	5 mg/mL (11.85 mM)
		Water	Insoluble
* <1 mg/ml means slightly soluble or insoluble. * Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

溶剤液（一定の濃度）を調合する

生物活性

製品説明	CCT251545 is a potent, orally bioavailable inhibitor of WNT signaling with IC50 of 5 nM in 7dF3 cells. CCT251545 also act as a selective chemical probe for exploring the role of CDK8 and CDK19 in human disease.
in vitro	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.^[1]
in vivo	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.^[1]

プロトコル(参考用のみ)

細胞アッセイ	細胞株	7dF3 cells, HEK293 cells, SW480, LS174T, COLO205 human colorectal cancer cells
	濃度	9.1 μM - 0.068 nM
	反応時間	2 h, 6 h
	実験の流れ	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.
動物実験	動物モデル	Female NMRI mice, Male Wistar rats
	投薬量	0.2 mg/kg, 0.5 mg/kg
	投与方法	IV, Oral gavage

参考

Selleckの高級品が、幾つかの出版された研究調査結果（以下を含む）で使われた：

Enhanced T cell effector activity by targeting the Mediator kinase module [ Science, 2022, 378(6620):eabn5647]	PubMed: 36356142
RING-Finger Protein 6 promotes Drug Resistance in Retinoblastoma via JAK2/STAT3 Signaling Pathway [ Pathol Oncol Res, 2022, 28:1610273]	PubMed: 35369571
Antagonizing CDK8 Sensitizes Colorectal Cancer to Radiation Through Potentiating the Transcription of e2f1 Target Gene apaf1 [ Front Cell Dev Biol, 2020, 8:408]	PubMed: 32596239

長期の保管のために-20°Cの下で製品を保ってください。

人間や獣医の診断であるか治療的な使用のためにでない。

各々の製品のための特定の保管と取扱い情報は、製品データシートの上で示されます。大部分のSelleck製品は、推薦された状況の下で安定です。製品は、推薦された保管温度と異なる温度で、時々出荷されます。長期の保管のために必要とされてそれと異なる温度で、多くの製品は、短期もので安定です。品質を維持するが、夜通しの積荷のために最も経済的な貯蔵状況を用いてあなたの送料を保存する状況の下に、製品が出荷されることを、我々は確実とします。製品の受領と同時に、製品データシートの上で貯蔵推薦に従ってください。