规格: | 98% |
分子量: | 406.44 |
包装 | 价格(元) |
5mg | 电议 |
10mg | 电议 |
25mg | 电议 |
Background:
EW-7195 is a potent and selective ALK5 (TGFβR1) inhibitor with an IC50 of 4.83 nM. EW-7195 has >300-fold selectivity for ALK5 over p38α. EW-7195 efficiently inhibits TGF-β1-induced Smad signaling, epithelial-to-mesenchymal transition (EMT) and breast tumour metastasis to the lung[1].
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[1].EW-7195 (0.5-1 µM; 1.5 hours) efficiently inhibits TGF-β1-induced Smad2 phosphorylation[1].
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[1].
[1]. Park CY, et al. EW-7195, a novel inhibitor of ALK5 kinase inhibits EMT and breast cancer metastasis to lung. Eur J Cancer. 2011;47(17):2642-2653.
Protocol:
ALK5 4.83nM(IC50) | p38α 1.5μM(IC50) |