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
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
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.
N-Bromosuccinimide Price
- Product number
- 19231
- Product name
- EW-7197
- Purity
- ≥98%
- Packaging
- 1mg
- Price
- $121
- Updated
- 2024/03/01
- Product number
- 19231
- Product name
- EW-7197
- Purity
- ≥98%
- Packaging
- 5mg
- Price
- $230
- Updated
- 2024/03/01
- Product number
- 19231
- Product name
- EW-7197
- Purity
- ≥98%
- Packaging
- 10mg
- Price
- $362
- Updated
- 2024/03/01
- Product number
- E950000
- Product name
- EW7197
- Packaging
- 100mg
- Price
- $945
- Updated
- 2021/12/16
- Product number
- 2408AH
- Product name
- EW-7197
- Packaging
- 100mg
- Price
- $967
- Updated
- 2021/12/16
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
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