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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 | USA Warehouse | Global Warehouse | Quantity |
|---|---|---|---|---|
| 1 mg | $30 | - | In Stock | |
| 5 mg | $64 | - | In Stock | |
| 10 mg | $98 | - | In Stock | |
| 25 mg | $163 | - | In Stock | |
| 50 mg | $255 | - | In Stock | |
| 100 mg | $396 | - | In Stock | |
| 200 mg | $579 | - | In Stock | |
| 1 mL x 10 mM (in DMSO) | $71 | - | In Stock |
| 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 | ALK2/4:17.3 nM, ALK5:12.9 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]. |
| Synonyms | TEW-7197 Hydrochloride, NOV1301 Hydrochloride, NOV 1301 Hydrochloride, EW-7197 Hydrochloride |
| Molecular Weight | 435.89 |
| Formula | C22H19ClFN7 |
| Cas No. | 1352610-25-3 |
| Smiles | Cl.FC=1C=CC=CC1NCC2=NC(C3=NC(=CC=C3)C)=C(N2)C=4C=CC5=NC=NN5C4 |
| 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/Shipping at ambient temperature. | ||||||||||||||||||||||||||||||||||||||||
| Solubility Information | H2O: 20 mg/mL (45.88 mM), Sonication is recommended. DMSO: 100 mg/mL (229.42 mM), Sonication is recommended. | ||||||||||||||||||||||||||||||||||||||||
| In Vivo Formulation | 10% DMSO+40% PEG300+5% Tween 80+45% Saline: 4 mg/mL (9.18 mM), Sonication is recommended. Please add the solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately. The formulation provided above is for reference purposes only. In vivo formulations may vary and should be modified based on specific experimental conditions. | ||||||||||||||||||||||||||||||||||||||||
Solution Preparation Table | |||||||||||||||||||||||||||||||||||||||||
H2O/DMSO
DMSO
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Dissolve 2 mg of the compound in 100 μL DMSO
to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.
1) Add 100 μL of the DMSO
stock solution to 400 μL PEG300
and mix thoroughly until the solution becomes clear.
2) Add 50 μL Tween 80 and mix well until fully clarified.
3) Add 450 μL Saline,PBS or ddH2O
and mix thoroughly until a homogeneous solution is obtained.
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