EW-7197 Hydrochloride
Modify Date: 2024-01-09 19:29:27
EW-7197 Hydrochloride structure
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Common Name | EW-7197 Hydrochloride | ||
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| CAS Number | 1352610-25-3 | Molecular Weight | 435.88 | |
| Density | N/A | Boiling Point | N/A | |
| Molecular Formula | C22H19ClFN7 | Melting Point | N/A | |
| MSDS | N/A | Flash Point | N/A | |
Use of EW-7197 HydrochlorideVactosertib Hydrochloride (EW-7197 Hydrochloride) is a small-molecule ATP-competitive inhibitor of TGFβRI (ALK5) with an IC50 of 12.9 nM. |
| Name | EW-7197 Hydrochloride |
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| Description | Vactosertib Hydrochloride (EW-7197 Hydrochloride) is a small-molecule ATP-competitive inhibitor of TGFβRI (ALK5) with an IC50 of 12.9 nM. |
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| Related Catalog | |
| Target |
IC50: 12.9 nM (ALK5)[1] |
| In Vitro | Kinase assays demonstrate that Vactosertib (EW-7197) is a small-molecule ATP-competitive inhibitor of TGFβRI (ALK5) with an IC50 of 12.9 nM. The IC50 values of Vactosertib against p38a is 1775 nM. Vactosertib also inhibits ACVR1B/ALK4 and the IC50 value against it is determined to be 17.3 nM. Vactosertib blocks the TGFβ-induced phosphorylation of Smad2 or Smad3 in a dose-dependent manner in 4T1 cells, and MDA-MB-231 cells. Vactosertib suppresses the TGFβ-induced nuclear translocation of Smad2/3 in 4T1 cells and MCF10A cells[1]. Vactosertib (EW-7197) treatment also dramatically reduces the colony-forming capacity of CML-MPPs in vitro in a dose-dependent manner[2]. |
| In Vivo | Vactosertib (EW-7197; 40 mg/kg) treatment of MMTV/c-Neu transgenic mice significantly reduces lung metastasis by 60% compare with the control. Treatment with Vactosertib decreases the number of metastatic nodules compare with that in the Veh-treated control group by 53% and 68% (5 and 20 mg/kg). Vactosertib (0.625, 1.25, 2.5, or 5 mg/kg; five times/week) inhibits lung metastasis and increases the survival of 4T1-Luc cells, in a dose-dependent manner. Vactosertib also prolongs the survival of BALB/c mice orthotopically bearing 4T1 tumors by 36% at doses of 2.5 and 5 mg/kg[1]. |
| Cell Assay | To determine colony-forming capacity after a combination treatment of Vactosertib plus IM, or Vactosertib plus ponatinib, freshly isolated CML-LICs on OP-9 stromal cells are cocultured in the presence of DMSO or Vactosertib for 24 h. Cells are then treated with additional DMSO, 1 μM IM, or 1 μM ponatinib and cultured for another 2 days (total, 3 days). Colonies are counted 7 days later[2]. |
| Animal Admin | BALB/c mice are used and maintained in a temperature-controlled room (at 21°C) and supplied with food and water. 4T1-luc cells are suspended in saline and injected into the tail veins of female BALB/c mice (50 μL/mouse; day 0). Artificial gastric fluid (Veh) or Vactosertib (0.625, 1.25, 2.5, or 5 mg/kg) dissolved in Veh is administered orally to mice five times per week from day 0 until death (n=13/group). On day 15, surviving mice are analyzed using an in vivo imaging system to compare metastases in the lungs. Luciferase-positive 4T1 cells are imaged with the IVIS-200 system. The captured images are quantified using the Living Image Software package[1]. |
| References |
| Molecular Formula | C22H19ClFN7 |
|---|---|
| Molecular Weight | 435.88 |