EW-7195

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

一种新型有效的选择性 TGF-βRI (ALK5) 抑制剂，IC50 为 4.83 nM。

A novel potent and selective TGF-βRI (ALK5) inhibitor with IC50 of 4.83 nM, dispalys >300-fold selectivity over p38α; decreases phosphorylated Smad2 levels and the nuclear translocation of Smad2 increased by TGF-β1, inhibits TGF-β1-induced epithelial-to-mesenchymal transition (EMT) and wound healing of NMuMG cells; inhibits metastasis to lung from breast tumours in xenografted mice.

EW7195 inhibits the EMT, motility, and invasiveness of breast cancer cells in vitro. EW-7195 efficiently blocks TGF-β1-induced phosphorylation of Smad2 followed by the nuclear translocation of Smad2/3. EW-7195 blocks TGF-β1-induced mesenchymal morphology. EW-7195 inhibits TGF-β-induced transcriptional activation.EW-7195 (0.5-1 μM; 1.5 hours) efficiently inhibits TGF-β1-induced Smad2 phosphorylation.

EW7195 (40 mg/kg; i.p.; three times a week for 3/2.5 weeks) inhibits lung metastasis development in both 4T1 orthotopic xenograft and MMTV/cNeu transgenic mice. Animal Model:MMTV/c-Neu mice Dosage:40 mg/kg Administration:I.p.; three times a week for 3 weeks Result:Inhibited the metastasis of breast cancer cells to the lung.Animal Model:Balb/c xenograft model (10-weeks-old female Balb/c mice bearing 4T1 cells)Dosage:40 mg/kg Administration:I.p.; three times a week for 2.5 weeks Result:Suppressed a lung metastasis in the Balb/c Xenograft model.

EW7195 | EW 7195

TGF-beta/Smad

TGFBR

TGFBR

——

——

1352609-28-9

406.453

C23H18N8

>98% (HPLC)

In Vitro:?DMSO : 50 mg/mL (123.02 mM)

——

3-[[[5-(6-Methyl-2-pyridinyl)-4-[1,2,4]triazolo[1,5-a]pyridin-6-yl-1H-imidazol-2-yl]methyl]amino]benzonitrile

(-20℃)

With Ice Pack

≥ 2 years