EW-7195 |
| Katalog-Nr.GC65329 |
EW-7195 ist ein potenter und selektiver ALK5 (TGFβR1)-Inhibitor mit einem IC50 von 4,83 nM. EW-7195 hat eine >300-fache SelektivitÄt fÜr ALK5 gegenÜber p38α. EW-7195 hemmt effizient die TGF-β1-induzierte Smad-SignalÜbertragung, den Übergang vom Epithel zum Mesenchym (EMT) und die Metastasierung von Brusttumoren in die Lunge.
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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