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Vactosertib Hydrochloride (EW-7197 Hydrochloride) is an orally active and highly efficient ATP-competitive ALK5 (activin receptor-like kinase 5) inhibitor, a TGF-β receptor I inhibitor with anti-metastatic and anticancer properties. It sensitizes pancreatic cancer cells to gemcitabine by inhibiting their viability.
Pack Size | Price | Availability | Quantity |
---|---|---|---|
2 mg | $78 | 5 days | |
5 mg | $102 | 5 days |
Description | Vactosertib Hydrochloride (EW-7197 Hydrochloride) is an orally active and highly efficient ATP-competitive ALK5 (activin receptor-like kinase 5) inhibitor, a TGF-β receptor I inhibitor with anti-metastatic and anticancer properties. It sensitizes pancreatic cancer cells to gemcitabine by inhibiting their viability. |
Targets&IC50 | ALK5:12.9 nM, ALK2/4:17.3 nM |
In vitro | Vactosertib Hydrochloride inhibits the TGFβ-induced nuclear translocation of Smad2/3 in 4T1 cells and MCF10A cells (IC50: 10-30 nM for Vactosertib Hydrochloride on pSmad3 in 4T1 cells). Vactosertib Hydrochloride (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 Hydrochloride abrogates TGFb1-induced tumor cell migration and invasion. Moreover, Vactosertib Hydrochloride abolishes the TGFβ1-induced effects on genes related to epithelial-to-mesenchymal transition (EMT)[2]. |
In vivo | Vactosertib Hydrochloride inhibits the epithelial-to-mesenchymal transition (EMT) in both TGFβ-treated breast cancer cells and 4T1 orthotopic-grafted mice. Vactosertib Hydrochloride (40 mg/kg; intraperitoneal injection; 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 Hydrochloride 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, NOV1301 Hydrochloride, NOV 1301 Hydrochloride, EW-7197 Hydrochloride |
Molecular Weight | 435.89 |
Formula | C22H19ClFN7 |
Cas No. | 1352610-25-3 |
Relative Density. | no data available |
Storage | keep away from moisture,store at low temperature | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | ||||||||||||||||||||||||||||||||||||||||
Solubility Information | H2O: 20 mg/mL (45.88 mM), Sonication is recommended. DMSO: 100 mg/mL (229.42 mM), Sonication is recommended. | ||||||||||||||||||||||||||||||||||||||||
Solution Preparation Table | |||||||||||||||||||||||||||||||||||||||||
H2O/DMSO
DMSO
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