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Pack Size | Price | Availability | Quantity |
---|---|---|---|
2 mg | $67 | 5 days | |
5 mg | $128 | 5 days |
Description | Vactosertib Hydrochloride is an orally active and ATP-competitive ALK5 inhibitor (IC50: 12.9 nM). It has potently antimetastatic activity and anticancer effect. Vactosertib Hydrochloride also inhibits ALK2 and ALK4 (IC50: 17.3 nM). |
Targets&IC50 | ALK5:12.9 nM |
In vitro | Vactosertib inhibits the TGFβ-induced nuclear translocation of Smad2/3 in 4T1 cells and MCF10A cells (IC50: 10-30 nM for Vactosertib on pSmad3 in 4T1 cells). Vactosertib (10-1000 nM; 30 minutes; 4T1 cells) treatment blocks the TGFβ-induced phosphorylation of Smad2 or Smad3 in a dose-dependent manner in 4T1 cells. Vactosertib abrogates TGFb1-induced tumor cell migration and invasion. Moreover, Vactosertib abolishes the TGFβ1-induced effects on genes related to epithelial-to-mesenchymal transition (EMT) [1]. |
In vivo | Vactosertib inhibits the epithelial-to-mesenchymal transition (EMT) in both TGFβ-treated breast cancer cells and 4T1 orthotopic-grafted mice. Vactosertib (40 mg/kg; i.p.; every other day; for 10 weeks; MMTV/c-Neu female mice) treatment inhibits Smad/TGFβ signaling, cell migration, invasion, and lung metastasis in MMTV/c-Neu mice. 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 [1]. |
Alias | TEW-7197 Hydrochloride, EW-7197 Hydrochloride |
Molecular Weight | 435.89 |
Formula | C22H19ClFN7 |
Cas No. | 1352610-25-3 |
Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | |||||||||||||||||||||||||||||||||||
Solubility Information | H2O: 50 mg/mL (114.71 mM), Sonication is recommended. DMSO: 50 mg/mL (114.71 mM), Sonication is recommended. | |||||||||||||||||||||||||||||||||||
Solution Preparation Table | ||||||||||||||||||||||||||||||||||||
H2O/DMSO
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