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Pack Size | Price | Availability | Quantity |
---|---|---|---|
2 mg | $39 | In Stock | |
5 mg | $64 | In Stock | |
10 mg | $97 | In Stock | |
25 mg | $163 | In Stock | |
50 mg | $255 | In Stock | |
100 mg | $393 | In Stock | |
200 mg | $582 | In Stock | |
500 mg | $913 | In Stock | |
1 g | $1,230 | In Stock | |
1 mL x 10 mM (in DMSO) | $70 | In Stock |
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 | ALK4:13 nM, ALK5:11 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] Vactosertib inhibits TGFβ-induced Smad2 or Smad3 phosphorylation and the epithelial-to-mesenchymal transition (EMT) in TGFβ-treated breast cancer cells. In addition, Vactosertib also abrogates TGFβ1-induced tumor cell migration and invasion in breast cells. [3] |
In vivo | In rats, Vactosertib 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. Vactosertib also shows low toxicity on the cardiovascular system, central nervous system, and respiratory system. [1] In a mouse B16 melanoma model, Vactosertib (2.5 mg/kg daily p.o.) suppresses the progression of melanoma with enhanced cytotoxic T-lymphocyte (CTL) responses. [2] Vactosertib 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) |
Alias | 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 | Shipping with blue ice. | |||||||||||||||||||||||||||||||||||
Solubility Information | H2O: < 1 mg/mL (insoluble or slightly soluble) Ethanol: 40 mg/mL (100.1 mM) DMSO: 60 mg/mL (150.22 mM) ![]() | |||||||||||||||||||||||||||||||||||
Solution Preparation Table | ||||||||||||||||||||||||||||||||||||
Ethanol/DMSO
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