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| | EW-7197 Basic information |
| Product Name: | EW-7197 | | Synonyms: | 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 | | CAS: | 1352608-82-2 | | MF: | C22H18FN7 | | MW: | 399.42 | | EINECS: | | | Product Categories: | Inhibitors;APIs | | Mol File: | 1352608-82-2.mol |  |
| | EW-7197 Chemical Properties |
| Melting point | >85oC (dec.) | | density | 1.40±0.1 g/cm3(Predicted) | | storage temp. | Refrigerator | | solubility | DMSO (Slightly), Methanol (Slightly) | | form | Solid | | pka | 8.51±0.10(Predicted) | | color | Pale Yellow to Light Yellow |
| | EW-7197 Usage And Synthesis |
| 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.
| | 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. | | 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.
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| | EW-7197 Preparation Products And Raw materials |
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