EW-7195

SKU: orb1691798

Description

EW-7195 is a potent and selective ALK5 (TGFβR1) inhibitor (IC50 = 4.83 nM) that effectively blocks TGF-β1-induced Smad signaling and EMT. It has demonstrated activity in inhibiting breast cancer metastasis to the lung in research models, supporting its use in studying fibrosis and cancer biology.

Research Area

Cardiovascular Research, Signal Transduction, Stem Cell & Developmental Biology

Key Properties

• CAS Number: 1352609-28-9
• MW: 406.44
• Purity: 99.98% (May vary between batches)
• Formula: C₂₃H₁₈N₈
• SMILES: Cc1cccc(n1)-c1[nH]c(CNc2cccc(c2)C#N)nc1-c1ccc2ncnn2c1
• Target: p38 MAPK,ALK,TGF-beta/Smad
• Solubility: DMSO:40 mg/mL (98.42 mM)

Bioactivity

• Target IC50:
  p38α:1.5 μM (IC50)|ALK5:4.83 nM (IC50)
• 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.
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• 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.
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Storage & Handling

• Storage: -20°C
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

Smad, TGF-beta/Smad, TGFbeta/Smad, TGF-beta, TGFbeta, TGF-β/Smad, TGFβ, TGF-b/Smad, TGFb, ALK5, EW 7195, EW-7195, EW7195

Compound Identifiers

PubChem CID

54767248