EW-7195 |
| カタログ番号GC65329 |
EW-7195 は、4.83 nM の IC50 を持つ強力かつ選択的な ALK5 (TGFβR1) 阻害剤です。 EW-7195 は、p38α よりも ALK5 に対して >300 倍の選択性があります。 EW-7195 は、TGF-β1 誘導性の Smad シグナル伝達、上皮間葉転換 (EMT)、および乳房腫瘍の肺への転移を効率的に阻害します。
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 1352609-28-9
Sample solution is provided at 25 µL, 10mM.
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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.
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