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EW-7197

Cat. No. M5246
EW-7197 Structure
Synonym:

Vactosertib; TEW-7197

Size Price Availability Quantity
10mM*1mL in DMSO USD 85  USD85 In stock
5mg USD 75  USD75 In stock
10mg USD 105  USD105 In stock
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Quality Control & Documentation
Biological Activity

In vitro: In HaCaT (3TP-luc) and 4T1 (3TP-luc) stable cells, 12b potently inhibits the TGF-β1-induced luciferase reporter activity with IC50 of 16.5 and 12.1 nM, respectively. EW-7197 inhibits TGFβ-induced Smad2 or Smad3 phosphorylation and the epithelial-to-mesenchymal transition (EMT) in TGFβ-treated breast cancer cells. In addition, EW-7197 also abrogates TGFβ1-induced tumor cell migration and invasion in breast cells. In vivo: In rats, EW-7197 shows an oral bioavailability of 51% with high systemic exposure (AUC) of 1426 ng×h/mL and maximum plasma concentration (Cmax) of 1620 ng/mL. EW-7197 also shows low toxicity on the cardiovascular system, central nervous system, and respiratory system. In a mouse B16 melanoma model, EW-7197 (2.5 mg/kg daily p.o.) suppresses the progression of melanoma with enhanced cytotoxic T-lymphocyte (CTL) responses. EW-7197 enhances cytotoxic T lymphocyte activity in 4T1 orthotopic-grafted mice and increased the survival time of 4T1-Luc and 4T1 breast tumor-bearing mice.

Protocol (for reference only)
Cell Experiment
Cell lines 4T1 and MCF10A cells
Preparation method Cells are seeded in 96 well plate and treated with indicated concentrations of EW-7197 in 0.2% HI-FBS medium for 72 h. Cells are dried after incubation with 10% TCA in media. Then, cells are incubated with 0.4% SRB (Sulforhodamine B) in 1% acetic acid for 30 min. After washing with 1% glacial acetic acid, bounded dye is released in 10 mM Tris buffer (pH 10.5) for 30 min. Absorbance is measured at 570 nm.
Concentrations ~5 μM
Incubation time 72 hours
Animal Experiment
Animal models Mouse B16 melanoma model
Formulation Artificial gastric fluid formulation (vehicle; ddH2O 900 mL, conc. HCl 7 mL, NaCl 2.0 g, pepsin 3.2 g).
Dosages 2.5 mg/kg daily
Administration p.o.
Chemical Information
Molecular Weight 399.42
Formula C22H18FN7
CAS Number 1352608-82-2
Solubility (25°C) DMSO 79 mg/mL
Storage Powder          -20°C   3 years ;  4°C   2 years
In solvent       -80°C   6 months ;  -20°C   1 month
Conversion of different model animals based on BSA (PMID: 27057123)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.

References

[1] Park SA, et al. Cell Mol Life Sci. EW-7197 inhibits hepatic, renal, and pulmonary fibrosis by blocking TGF-β/Smad and ROS signaling.

[2] Son JY, et al. Mol Cancer Ther. EW-7197, a novel ALK-5 kinase inhibitor, potently inhibits breast to lung metastasis.

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Keywords: EW-7197, Vactosertib; TEW-7197 supplier, TGF-β Receptor, inhibitors, activators


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