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Vactosertib Hydrochloride

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Catalog No. T15262Cas No. 1352610-25-3
Alias TEW-7197 Hydrochloride, EW-7197 Hydrochloride

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).

Vactosertib Hydrochloride

Vactosertib Hydrochloride

😃Good
Catalog No. T15262Alias TEW-7197 Hydrochloride, EW-7197 HydrochlorideCas No. 1352610-25-3
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).
Pack SizePriceAvailabilityQuantity
2 mg$785 days
5 mg$1025 days
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Product Introduction

Bioactivity
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].
AliasTEW-7197 Hydrochloride, EW-7197 Hydrochloride
Chemical Properties
Molecular Weight435.89
FormulaC22H19ClFN7
Cas No.1352610-25-3
Relative Density.no data available
Storage & Solubility Information
StoragePowder: -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
1mg5mg10mg50mg
1 mM2.2942 mL11.4708 mL22.9416 mL114.7078 mL
5 mM0.4588 mL2.2942 mL4.5883 mL22.9416 mL
10 mM0.2294 mL1.1471 mL2.2942 mL11.4708 mL
20 mM0.1147 mL0.5735 mL1.1471 mL5.7354 mL
50 mM0.0459 mL0.2294 mL0.4588 mL2.2942 mL
100 mM0.0229 mL0.1147 mL0.2294 mL1.1471 mL

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Preparation method for in vivo formula: Take 50 μL DMSOTargetMol | reagent main solution, add 300 μLPEG300TargetMol | reagent mix well and clarify, then add 50 more μL Tween 80, mix well and clarify, then add 600 more μLddH2OTargetMol | reagent mix well and clarify
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