1. TGF-beta/Smad
  2. TGF-β Receptor

EW-7197 

Cat. No.: HY-19928 Purity: 99.12%
Data Sheet SDS Handling Instructions

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.

For research use only. We do not sell to patients.
EW-7197 Chemical Structure

EW-7197 Chemical Structure

CAS No. : 1352608-82-2

Size Price Stock Quantity
Free Sample (0.5-1 mg)   Apply now  
10 mM * 1 mL in DMSO $114 In-stock
2 mg $90 In-stock
5 mg $130 In-stock
10 mg $220 In-stock
25 mg $440 In-stock
50 mg $680 In-stock
100 mg $950 In-stock
200 mg   Get quote  
500 mg   Get quote  

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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. target: ALK4/ALK5 IC 50: 13 nM for TGF-β receptor ALK4, 11 nM for TGF-β receptor ALK5. [1] In vitro: 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. EW-7197 inhibited Smad/TGFβ signaling, cell migration, invasion, and lung metastasis in mouse mammary tumor virus. [2] In vivo: EW-7197 inhibition downregulates Smad4 in melanoma-bearing mice. EW-7197 induces ubiquitin-mediated degradation of Smad4 in melanoma-bearing mice. 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. EW-7197 dissolved in artificial gastric fluid formulation (vehicle; ddH2O 900 ml, conc. HCl 7 ml, NaCl 2.0 g, pepsin 3.2 g) was given orally by feeding needle to mice from 4 days after inoculation. [3]

Clinical Trial
NCT Number Sponsor Condition Start Date Phase
NCT02160106 MedPacto, Inc.|National OncoVenture Advanced Stage Solid Tumors June 2014 Phase 1
NCT03143985 Case Comprehensive Cancer Center Multiple Myeloma July 2017 Phase 1
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References
M.Wt

399.42

Formula

C₂₂H₁₈FN₇

CAS No.

1352608-82-2

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Shipping

Room temperature in continental US; may vary elsewhere

Solvent & Solubility

10 mM in DMSO

* "<1 mg/mL" means slightly soluble or insoluble. "≥" means soluble, but saturation unknown.

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EW-7197
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HY-19928
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