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Vactosertib Hydrochloride

Vactosertib Hydrochloride
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Vactosertib Hydrochloride

Catalog No. T15262Cas 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).
All TargetMol products are for research purposes only and cannot be used for human consumption. We do not provide products or services to individuals. Please comply with the intended use and do not use TargetMol products for any other purpose.
Pack SizePriceAvailabilityQuantity
2 mg$675 days
5 mg$1285 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
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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Mother liquor preparation method: 2 mg of drug dissolved in 50 μL DMSOTargetMol | reagent (mother liquor concentration of 40 mg/mL), if you need to configure a concentration that exceeds the solubility of the product, please contact us first.
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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