EW-7195

EW-7195 is a potent and selective ALK5 (TGFβR1) inhibitor with an IC 50 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 In Vitro 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. MCE has not independently confirmed the accuracy of these methods. They are for reference only. In Vivo 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 . MCE has not independently confirmed the accuracy of these methods. They are for reference only. 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. IC50& Target:ALK5 4.83 nM (IC 50 ) p38α 1.5 μM (IC 50 )

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