ChemicalBook > CAS DataBase List > EW-7197

EW-7197

Product Name
EW-7197
CAS No.
1352608-82-2
Chemical Name
EW-7197
Synonyms
CS-2287;CS-2288;EW-7197;CPD3325;EW-7179;TEW-7197;NOV-1301;CPD3325-A5;Vactosertib;EW-7197 (EW7197
CBNumber
CB42729651
Molecular Formula
C22H18FN7
Formula Weight
399.42
MOL File
1352608-82-2.mol
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EW-7197 Property

Melting point:
>85oC (dec.)
Density 
1.40±0.1 g/cm3(Predicted)
storage temp. 
Refrigerator
solubility 
DMSO (Slightly), Methanol (Slightly)
pka
8.51±0.10(Predicted)
form 
Solid
color 
Pale Yellow to Light Yellow
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Hazard and Precautionary Statements (GHS)

Symbol(GHS)
Signal word
Warning
Hazard statements

H315Causes skin irritation

H319Causes serious eye irritation

H335May cause respiratory irritation

Precautionary statements

P261Avoid breathing dust/fume/gas/mist/vapours/spray.

P305+P351+P338IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continuerinsing.

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N-Bromosuccinimide Price

Cayman Chemical
Product number
19231
Product name
EW-7197
Purity
≥98%
Packaging
1mg
Price
$121
Updated
2024/03/01
Cayman Chemical
Product number
19231
Product name
EW-7197
Purity
≥98%
Packaging
5mg
Price
$230
Updated
2024/03/01
Cayman Chemical
Product number
19231
Product name
EW-7197
Purity
≥98%
Packaging
10mg
Price
$362
Updated
2024/03/01
TRC
Product number
E950000
Product name
EW7197
Packaging
100mg
Price
$945
Updated
2021/12/16
Biosynth Carbosynth
Product number
BT168124
Product name
TEW 7197
Packaging
10mg
Price
$70
Updated
2021/12/16
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EW-7197 Chemical Properties,Usage,Production

Description

EW-7197 is a potent inhibitor of activin receptor-like kinase 5 (ALK5, also known as TGF-β receptor type 1; IC50 = 12.9 nM). It also inhibits ALK2 and ALK4 at nanomolar concentrations. EW-7197 blocks TGF-β/Smad signaling, cell migration, invasion, and lung metastasis in mouse mammary tumor virus/c-Neu mice and 4TI orthotopic-grafted mice. It also inhibits epithelial-to-mesenchymal transition (EMT) in TGF-β-treated breast cancer cells. EW-7197 is used to block TGF-β signaling and EMT in animal models of cancer and fibrosis.

Description

EW-7197 is a novel ALK-5 kinase inhibitor as well as TGF-β Type I Receptor Kinase Inhibitor. Study has shown that it can potently inhibit the breast to lung metastasis. Mice study has demonstrated that EW-7197 inhibited Smad/TGFβ signaling, cell migration, invasion, and lung metastasis in MMTV/c-Neu mice and 4T1 orthotopic-grafted mice. EW-7197 also inhibited the epithelial-to-mesenchymal transition (EMT) in both TGFβ-treated breast cancer cells and 4T1 orthotopic-grafted mice. Furthermore, EW-7197 enhanced cytotoxic T lymphocyte activity in 4T1 orthotopic-grafted mice and increased the survival time of 4T1-Luc and 4T1 breast tumor-bearing mice. It can also inhibit hepatic, renal, and pulmonary fibrosis by blocking TGF-β/Smad and ROS signaling. Therefore, it is a potential antitumor reagent.

Uses

EW-7197 is a highly potent, selective, and orally bioavailable TGF-β I receptor ALK4/ALK5 inhibitor.

in vitro

ew-7197 inhibited alk5 with ic50 value of 0.013 μm in a kinase assay and with ic50 values of 0.0165 and 0.0121 μm in hacat stable cells and 4t1 stable cells, respectively, in a luciferase assay. selectivity profiling of ew-7197 using a panel of protein kinases revealed that it is a highly selective alk5/alk4 inhibitor [1].

in vivo

ew-7197 inhibited smad/tgf-βsignaling, invasion, cell migration, and lung metastasis in mmtv/c-neu mice and 4t1 orthotopic–grafted mice. ew-7197 inhibited the epithelial-to-mesenchymal transition in both tgf-β-treated breast cancer cells and 4t1 orthotopic–grafted mice as well[2].

IC 50

0.013 μm

References

Park, S. A., et al. "EW-7197 inhibits hepatic, renal, and pulmonary fibrosis by blocking TGF-β/Smad and ROS signaling." Cellular & Molecular Life Sciences 72.10(2015):2023-2039.
Kim, Min Jin, et al. "TGF-β Type I Receptor Kinase Inhibitor EW-7197 Suppresses Cholestatic Liver Fibrosis by Inhibiting HIF1α-Induced Epithelial Mesenchymal Transition." Cellular Physiology & Biochemistry International Journal of Experimental Cellular Physiology Biochemistry & Pharmacology 38.2(2016):571.
Son, J. Y., et al. "EW-7197, a novel ALK-5 kinase inhibitor, potently inhibits breast to lung metastasis." Molecular Cancer Therapeutics13.7(2014):1704.

EW-7197 Preparation Products And Raw materials

Raw materials

Preparation Products

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EW-7197 Suppliers

A.J Chemicals
Tel
--
Fax
--
Email
sales@ajchem.in
Country
India
ProdList
6100
Advantage
58

1352608-82-2, EW-7197Related Search:


  • EW-7197
  • Vactosertib (EW-7197
  • CS-2287
  • EW-7197 (EW7197
  • CS-2288
  • MK-4101 (MK 4101
  • EW-7197;EW 7197;EW7197;TEW-7197; NOV-1301
  • N-(2-fluorophenyl)-5-(6-methyl-2-pyridinyl)-4-[1,2,4]triazolo[1,5-a]pyridin-6-yl-1H-imidazole-2-methanamine
  • NOV-1301
  • TEW-7197
  • N-[[4-([1,2,4]Triazolo[1,5-a]pyridin-6-yl)-5-(6-methylpyridin-2-yl)-1H-imidazol-2-yl]methyl]-2-fluoroaniline
  • CPD3325-A5
  • N-(2-Fluorophenyl)-5-(6-methyl-2-pyridinyl)-4-[1,2,4]triazolo-[1,5-a]pyridin-6-yl-1H-imidazole
  • CPD3325
  • 1H-Imidazole-2-methanamine, N-(2-fluorophenyl)-5-(6-methyl-2-pyridinyl)-4-[1,2,4]triazolo[1,5-a]pyridin-6-yl-
  • Vactosertib
  • Vactosertib (Synonyms: EW-7197
  • Vactosertib (TEW-7197)
  • N-[[4-([1,2,4]Triazolo[1,5-a]pyridin-6-yl)-5-(6-methyl-2-pyridyl)-2-imidazolyl]methyl]-2-fluoroaniline
  • EW-7197 Vactosertib
  • EW-7197 USP/EP/BP
  • EW-7179
  • TEW-7197EW 7197
  • 1352608-82-2
  • C22H18FN7
  • Inhibitors
  • APIs