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编 号:F682862
分子式:C23H18N8
分子量:406.44
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10mM*1mL in DMSO
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1mg
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5mg
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10mg
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生物活性:
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.

体内研究:
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.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.

体外研究:
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.
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