EW-7195

EW-7195CAS号: 1352609-28-9分子式: C23H18N8分子量: 406.44描述储存/保存方法可溶性/溶解性靶点In vitro(体外研究)In vivo(体内研究)

产品描述
描述
EW-7195 is a selective and potent inhibitor of ALK5 (TGFβR1) with an IC50 value of 4.83 nM.EW-7195 has an affinity for ALK5 that is more than 300-fold higher than that of p38α.EW-7195 has an inhibitory effect on TGF-β1-induced Smad signaling, epithelial mesenchymal transition (EMT), and breast cancer metastasis to the lungs.
储存/保存方法
Store at -20℃ for one year(Powder);Store at 2-4℃ for two weeks;Store at -20℃ for six months after dissolution.
基本信息
可溶性/溶解性
DMSO:40 mg/mL (98.42 mM)
生物活性
靶点
p38α:1.5 μM (IC50), ALK5:4.83 nM (IC50)
In vitro(体外研究)
In vitro, EW-7195 efficiently inhibits the epithelial-to-mesenchymal transition (EMT), motility, and invasiveness of breast cancer cells. Following a 1.5-hour treatment at concentrations of 0.5-1 µM, EW-7195 effectively blocks TGF-β1-induced phosphorylation of Smad2, subsequently preventing the nuclear translocation of Smad2/3. Additionally, EW-7195 hinders TGF-β1-induced mesenchymal morphology and transcriptional activation[1].
In vivo(体内研究)
In both 4T1 orthotopic xenograft and MMTV/cNeu transgenic mice, EW7195 (40 mg/kg; intraperitoneal; three times a week for 3/2.5 weeks) inhibits the development of lung metastasis[1].