Home TGF-beta/Smad TGF-beta/Smad inhibitor Vactosertib (TEW-7197) For research use only.

Vactosertib (TEW-7197)

Synonyms: EW-7197

Vactosertib  (TEW-7197, 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.

Vactosertib (TEW-7197) Chemical Structure

Vactosertib (TEW-7197) Chemical Structure

CAS No. 1352608-82-2

Purity & Quality Control

Vactosertib (TEW-7197) Related Products

Signaling Pathway

TGF-beta/Smad Signaling Pathways

TGF-beta/Smad Signaling Pathway

Cell Data

Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
Sf9 Function assay Inhibition of human recombinant ALK5 expressed in insect Sf9 cells using casein as substrate by radioisotopic assay, IC50 = 0.007 μM. 24786585
Sf9 Function assay Inhibition of human recombinant GST-fused ALK5 expressed in Sf9 insect cells using casein as substrate by proprietary radioisotopic protein kinase assay, IC50 = 0.00967 μM. 26483198
4T1 Function assay 24 hrs Inhibition of ALK5 in mouse 4T1 cells assessed as inhibition of TGFbeta1-induced luciferase activity after 24 hrs by luciferase reporter gene assay, IC50 = 0.0121 μM. 24786585
HaCaT Function assay 24 hrs Inhibition of ALK5 in human HaCaT cells assessed as inhibition of TGFbeta1-induced luciferase activity after 24 hrs by luciferase reporter gene assay, IC50 = 0.0165 μM. 24786585
HEK293 Function assay 3 to 5.7 mins Inhibition of human ERG channel expressed in HEK293 cells after 3 to 5.7 mins by whole-cell patch clamp technique, IC50 = 31.04 μM. 24786585
B16 Antitumor assay 2.5 mg/kg Antitumor activity against mouse B16 cells in mouse assessed as suppression of tumor volume at 2.5 mg/kg, po qd relative to vehicle-treated control 24786585
B16 Antitumor assay 2.5 mg/kg Antitumor activity against mouse B16 cells in mouse assessed as inhibition of tumor growth at 2.5 mg/kg, po qd relative to vehicle-treated control 24786585
B16 Antitumor assay 2.5 mg/kg Antitumor activity against mouse B16 cells in mouse assessed as inhibition of lymph node metastasis at 2.5 mg/kg, po qd relative to vehicle-treated control 24786585
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Biological Activity

Description Vactosertib  (TEW-7197, 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 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]
Kinase Assay Protein Kinase Assay
A radioisotopic protein kinase assay (HotSpot assay) is performed at Reaction Biology Corporation.
Cell Research 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.
Experimental Result Images Methods Biomarkers Images PMID
Western blot α-CUG2 / α-E-cadherin / α-N-cadherin / α-vimentin α-p-Smad2 / α-Smad2/3 / α-Twist / α-Snail α-p-AKT / α-AKT / α-p-ERK / α-ERK / α-p-JNK / α-JNK / α-p-p38 / α-p38 27974707
Immunofluorescence Smad2 / Smad3 31496148
In Vivo
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]
Animal Research Animal Models Mouse B16 melanoma model
Dosages 2.5 mg/kg daily
Administration p.o.

Chemical Information & Solubility

Molecular Weight 399.42 Formula

C22H18FN7
CAS No. 1352608-82-2 SDF Download Vactosertib (TEW-7197) SDF
Smiles CC1=NC(=CC=C1)C2=C(N=C(N2)CNC3=CC=CC=C3F)C4=CN5C(=NC=N5)C=C4
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 79 mg/mL ( (197.78 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 79 mg/mL

Water : Insoluble


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In vivo
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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

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