EW-7195 是一种有效的、选择性 ALK5 (TGFβR1) 抑制剂，IC50 为 4.83 nM。EW-7195 对 ALK5 的选择性是 p38α 的 300 多倍。EW-7195 能有效抑制 TGF-β1 诱导的 Smad 信号转导、上皮间质转化 (EMT) 和乳腺癌向肺转移。
货号:ajcx39368
CAS:1352609-28-9
分子式:C23H18N8
分子量：406.44
溶解度:DMSO : 50 mg/mL (123.02 mM; Need ultrasonic)
纯度：98%
存储：Store at -20°C
库存：现货

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)