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Vactosertib

Catalog No. T6496   CAS 1352608-82-2
Synonyms: TEW-7197, EW-7197

Vactosertib (EW-7197) is an orally bioavailable inhibitor of the serine/threonine kinase, transforming growth factor (TGF)-beta receptor type 1 (TGFBR1), also known as activin receptor-like kinase 5 (ALK5), with potential antineoplastic activity.

All products from TargetMol are for Research Use Only. Not for Human or Veterinary or Therapeutic Use.
Vactosertib Chemical Structure
Vactosertib, CAS 1352608-82-2
Pack Size Availability Price/USD Quantity
2 mg In stock $ 39.00
5 mg In stock $ 64.00
10 mg In stock $ 97.00
25 mg In stock $ 163.00
50 mg In stock $ 255.00
100 mg In stock $ 393.00
200 mg In stock $ 582.00
500 mg In stock $ 913.00
1 g In stock $ 1,230.00
1 mL * 10 mM (in DMSO) In stock $ 70.00
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Purity: 99.81%
Purity: 99.78%
Purity: 99.55%
Purity: 99.43%
Purity: 98.85%
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Biological Description
Chemical Properties
Storage & Solubility Information
Description Vactosertib (EW-7197) is an orally bioavailable inhibitor of the serine/threonine kinase, transforming growth factor (TGF)-beta receptor type 1 (TGFBR1), also known as activin receptor-like kinase 5 (ALK5), with potential antineoplastic activity.
Targets&IC50 ALK5:11 nM, ALK4:13 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]
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]
Kinase Assay Protein Kinase Assay: A radioisotopic protein kinase assay (HotSpot assay) is performed at Reaction Biology Corporation.
Cell Research 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)
Synonyms TEW-7197, EW-7197
Molecular Weight 399.42
Formula C22H18FN7
CAS No. 1352608-82-2

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

H2O: < 1 mg/mL (insoluble or slightly soluble)

Ethanol: 40 mg/mL (100.1 mM)

DMSO: 73 mg/mL (182.8 mM)

TargetMolReferences and Literature

1. Jin CH, et al. J Med Chem. 2014, 57(10), 4213-4238. 2. Yoon JH, et al. EMBO Mol Med. 2013, 5(11), 1720-1739. 3. Son JY, et al. Mol Cancer Ther. 2014, 13(7), 1704-1716. 4. Kalli M, Mpekris F, Wong C K, et al. Activin A signaling regulates IL13Rα2 expression to promote breast cancer metastasis[J]. Frontiers in oncology. 2019 Feb 5;9:32.

TargetMolCitations

1. Kalli M, Mpekris F, Wong C K, et al. Activin A signaling regulates IL13Rα2 expression to promote breast cancer metastasis. Frontiers in Oncology. 2019 Feb 5;9:32

Related compound libraries

This product is contained In the following compound libraries:
Anti-Cancer Clinical Compound Library Anti-Cancer Drug Library Tyrosine Kinase Inhibitor Library Anti-Cancer Active Compound Library TGF-beta/Smad Compound Library Cytokine Inhibitor Library Anti-Fibrosis Compound Library Anti-COVID-19 Compound Library Fluorochemical Library Orally Active Compound Library

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Keywords

Vactosertib 1352608-82-2 Angiogenesis Stem Cells Tyrosine Kinase/Adaptors ALK TGF-beta/Smad antimetastatic invasion Smad Transforming growth factor beta receptors TGFβ TEW 7197 migration TGF-β Receptor breast TEW-7197 inhibit cell EW7197 TEW7197 cancer survival EW 7197 EW-7197 Inhibitor p38α inhibitor

 

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