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EW-7195 is a selective and potent inhibitor of ALK5 (TGFβR1) with an IC50 value of 4.83 nM.EW-7195 has an affinity for ALK5 that is more than 300-fold higher than that of p38α.EW-7195 has an inhibitory effect on TGF-β1-induced Smad signaling, epithelial mesenchymal transition (EMT), and breast cancer metastasis to the lungs.
Pack Size | Price | Availability | Quantity |
---|---|---|---|
1 mg | $133 | In Stock | |
2 mg | $196 | In Stock | |
5 mg | $328 | In Stock | |
10 mg | $563 | In Stock | |
25 mg | $1,120 | In Stock | |
50 mg | $1,830 | In Stock | |
100 mg | $2,890 | In Stock | |
1 mL x 10 mM (in DMSO) | $363 | In Stock |
Description | EW-7195 is a selective and potent inhibitor of ALK5 (TGFβR1) with an IC50 value of 4.83 nM.EW-7195 has an affinity for ALK5 that is more than 300-fold higher than that of p38α.EW-7195 has an inhibitory effect on TGF-β1-induced Smad signaling, epithelial mesenchymal transition (EMT), and breast cancer metastasis to the lungs. |
Targets&IC50 | p38α:1.5 μM (IC50), ALK5:4.83 nM (IC50) |
In vitro | In vitro, EW-7195 efficiently inhibits the epithelial-to-mesenchymal transition (EMT), motility, and invasiveness of breast cancer cells. Following a 1.5-hour treatment at concentrations of 0.5-1 µM, EW-7195 effectively blocks TGF-β1-induced phosphorylation of Smad2, subsequently preventing the nuclear translocation of Smad2/3. Additionally, EW-7195 hinders TGF-β1-induced mesenchymal morphology and transcriptional activation[1]. |
In vivo | In both 4T1 orthotopic xenograft and MMTV/cNeu transgenic mice, EW7195 (40 mg/kg; intraperitoneal; three times a week for 3/2.5 weeks) inhibits the development of lung metastasis[1]. |
Molecular Weight | 406.44 |
Formula | C23H18N8 |
Cas No. | 1352609-28-9 |
Smiles | Cc1cccc(n1)-c1[nH]c(CNc2cccc(c2)C#N)nc1-c1ccc2ncnn2c1 |
Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | ||||||||||||||||||||||||||||||
Solubility Information | DMSO: 40 mg/mL (98.42 mM), Sonication is recommended. | ||||||||||||||||||||||||||||||
Solution Preparation Table | |||||||||||||||||||||||||||||||
DMSO
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