1. TGF-beta/Smad
    MAPK/ERK Pathway
  2. TGF-β Receptor
    p38 MAPK
  3. EW-7195

EW-7195 

Cat. No.: HY-18766
Handling Instructions

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.

For research use only. We do not sell to patients.

EW-7195 Chemical Structure

EW-7195 Chemical Structure

CAS No. : 1352609-28-9

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Description

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].

IC50 & Target[1]

ALK5

4.83 nM (IC50)

p38α

1.5 μM (IC50)

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[1].
EW-7195 (0.5-1 µM; 1.5 hours) efficiently inhibits TGF-β1-induced Smad2 phosphorylation[1].

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[1].

Animal Model: MMTV/c-Neu mice[1]
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)[1]
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.
Molecular Weight

406.44

Formula

C₂₃H₁₈N₈

CAS No.

1352609-28-9

SMILES

N#CC1=CC=CC(NCC2=NC(C3=CN4C(C=C3)=NC=N4)=C(C5=NC(C)=CC=C5)N2)=C1

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Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

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Keywords:

EW-7195EW7195EW 7195TGF-β Receptorp38 MAPKTransforming growth factor beta receptorsEMTmotilityinvasivenessbreastphosphorylationSmad2morphologycancerlungInhibitorinhibitorinhibit

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