EW-7197

Bezeichnung:EW-7197

CAS-Nr1352608-82-2

Englisch Name:EW-7197

CBNumberCB42729651

SummenformelC22H18FN7

Molgewicht399.42

MOL-Datei1352608-82-2.mol

EW-7197 physikalisch-chemischer Eigenschaften

Schmelzpunkt	>85oC (dec.)
Dichte	1.40±0.1 g/cm3(Predicted)
storage temp.	Refrigerator
Löslichkeit	DMSO (Slightly), Methanol (Slightly)
pka	8.51±0.10(Predicted)
Aggregatzustand	Solid
Farbe	Pale Yellow to Light Yellow

Gefahreninformationscode (GHS)

EW-7197 Chemische Eigenschaften,Einsatz,Produktion Methoden

Beschreibung
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.
Beschreibung
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.
Verwenden
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
Einzelnachweise
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 Anbieter Lieferant Produzent Hersteller Vertrieb Händler.

Send Inquriy