1-(4-Chloro-3-(trifluoromethyl)phenyl)-3-(4-(4-cyanophenoxy)phenyl)urea

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Chemical Structure| 1313019-65-6 同义名 : SC-1; STAT3-IN-7; CHEMBL1796725; 1-[4-chloro-3-(trifluoromethyl)phenyl]-3-[4-(4-cyanophenoxy)phenyl]urea
CAS号 : 1313019-65-6
货号 : A1326050
分子式 : C21H13ClF3N3O2
纯度 : 99%+
分子量 : 431.8
MDL号 : MFCD27665015
存储条件:

Pure form Sealed in dry,2-8°C

In solvent -20°C:3-6个月-80°C:12个月

溶解度 : -
动物实验配方:
生物活性
描述 The signal transducer and activator of transcription 3 (STAT3) is a transcription factor associated with liver injury, inflammation, and regeneration. SC-1 (which is STAT3-IN-7), an aryl sulfonamide azetidine compound, is an orally active STAT3 inhibitor. It is a derivative of the multiple tyrosine kinase inhibitor sorafenib, blocks STAT3 phosphorylation and activation, and induces apoptosis in hepatocellular carcinoma cell lines, and has anticancer activities. SC-1 had dose- and time-dependent effects against cell viability on HSC-T6, LX2, and mouse primary hepatic stellate cells (HSCs). Further, SC-1 down-regulated p-STAT3 and suppressed Mcl-1 and cyclin D1 in both HSC-T6 and LX2 cell lines in a dose-dependent manner. Moreover, SC-1–induced apoptosis was abolished in STAT3-overexpressing HSC cells. In hepatotoxic and cholestatic models, hepatic fibrosis significantly reduced after SC-1 treatment in terms of Metavir fibrosis score and collagen-positive area[2].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.32mL

0.46mL

0.23mL

11.58mL

2.32mL

1.16mL

23.16mL

4.63mL

2.32mL

参考文献

[1]Chun-Yu Liu, et al. Novel sorafenib analogues induce apoptosis through SHP-1 dependent STAT3 inactivation in human breast cancer cells. Breast Cancer Res. 2013;15(4):R63.

[2]Su TH, Shiau CW, Jao P, Liu CH, Liu CJ, Tai WT, Jeng YM, Yang HC, Tseng TC, Huang HP, Cheng HR, Chen PJ, Chen KF, Kao JH, Chen DS. Sorafenib and its derivative SC-1 exhibit antifibrotic effects through signal transducer and activator of transcription 3 inhibition. Proc Natl Acad Sci U S A. 2015 Jun 9;112(23):7243-8.