EW-7197

Catalog No.S7530

EW-7197 Chemical Structure

Molecular Weight(MW): 399.42

EW-7197 is a highly potent, selective, and orally bioavailable TGF-β receptor ALK4/ALK5 inhibitor with IC50 of 13 nM and 11 nM, respectively. Phase 1.

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USD 197 In stock
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1 Customer Review

  • Representative immunofluorescent images of HuL6 cells treated with EW-7197, TGF-β1, both, or neither for 72 h. Scale bars, 20 μm.

    Lab Invest, 2017, 97(3):232-242. EW-7197 purchased from Selleck.

Purity & Quality Control

Choose Selective TGF-beta/Smad Inhibitors

Biological Activity

Description EW-7197 is a highly potent, selective, and orally bioavailable TGF-β receptor ALK4/ALK5 inhibitor with IC50 of 13 nM and 11 nM, respectively. Phase 1.
Targets
ALK5 [1]
(Cell-free assay)
ALK4 [1]
(Cell-free assay)
11 nM 13 nM
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. [1] 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. [3]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
mouse 4T1 cells M2TQRmZ2dmO2aX;uJIF{e2G7 NFXmc2kzPCCq NF;LfnJKdmirYnn0bY9vKG:oIFHMT|UhcW5ibX;1d4UhPFRzIHPlcIx{KGG|c3Xzd4VlKGG|IHnubIljcXSrb36gc4YhXEeIYnX0ZVEucW6mdXPl[EBtfWOrZnXyZZNmKGGldHn2bZR6KGGodHXyJFI1KGi{czDifUBtfWOrZnXyZZNmKHKncH;yeIVzKGenbnWgZZN{[XluIFnDOVA:OC5yMUKxJO69VQ>? NX;LRWRSOjR5OE[1PFU>
human HaCaT cells M3L4UWZ2dmO2aX;uJIF{e2G7 MWCyOEBp NHi3NnlKdmirYnn0bY9vKG:oIFHMT|UhcW5iaIXtZY4hUGGFYWSgZ4VtdHNiYYPz[ZN{\WRiYYOgbY5pcWKrdHnvckBw\iCWR1\i[ZRiOS2rbnT1Z4VlKGy3Y3nm[ZJie2ViYXP0bZZqfHliYX\0[ZIhOjRiaILzJIJ6KGy3Y3nm[ZJie2VicnXwc5J1\XJiZ3Xu[UBie3OjeTygTWM2OD1yLkCxOlUh|ryP M{fHRVI1Pzh4NUi1
HEK293 cells NYnB[ZpJTnWwY4Tpc44h[XO|YYm= NVTvWo1YUW6qaXLpeIlwdiCxZjDoeY1idiCHUlegZ4hidm6nbDDlfJBz\XO|ZXSgbY4hUEWNMkmzJINmdGy|IHHmeIVzKDNidH:gOU44KG2rboOgZpkhf2ixbHWtZ4VtdCCyYYTjbEBkdGGvcDD0[YNpdmmzdXWsJGlEPTB;M{GuNFQh|ryP MkPSNlQ4QDZ3OEW=

... Click to View More Cell Line Experimental Data

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. [1] 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. [2] 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. [3]

Protocol

Kinase Assay:

[1]

+ Expand

Protein Kinase Assay:

A radioisotopic protein kinase assay (HotSpot assay) is performed at Reaction Biology Corporation.
Cell Research:

[3]

+ Expand
  • Cell lines: 4T1 and MCF10A cells
  • Concentrations: ~5 μM
  • Incubation Time: 72 hours
  • 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.


    (Only for Reference)
Animal Research:

[2]

+ Expand
  • 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.
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 79 mg/mL (197.78 mM)
Ethanol 43 mg/mL (107.65 mM)
Water Insoluble

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 399.42
Formula

C22H18FN7

CAS No. 1352608-82-2
Storage powder
Synonyms N/A

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Clinical Trial Information

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT02160106 Recruiting Advanced Stage Solid Tumors MedPacto, Inc.|National OncoVenture June 2014 Phase 1

Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

Tel: +1-832-582-8158 Ext:3

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID