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Vactosertib Hydrochloride

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Catalog No. T15262Cas No. 1352610-25-3
Alias TEW-7197 Hydrochloride, NOV1301 Hydrochloride, NOV 1301 Hydrochloride, EW-7197 Hydrochloride

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.

Vactosertib Hydrochloride

Vactosertib Hydrochloride

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Purity: 98.03%
Catalog No. T15262Alias TEW-7197 Hydrochloride, NOV1301 Hydrochloride, NOV 1301 Hydrochloride, EW-7197 HydrochlorideCas No. 1352610-25-3
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 SizePriceUSA WarehouseGlobal WarehouseQuantity
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
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In Stock Estimated shipping dateUSA Warehouse[1-2 days] Global Warehouse[5-7 days]
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.
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Purity:98.03%
Appearance:Solid
Color:White
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Product Introduction

Bioactivity
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].
SynonymsTEW-7197 Hydrochloride, NOV1301 Hydrochloride, NOV 1301 Hydrochloride, EW-7197 Hydrochloride
Chemical Properties
Molecular Weight435.89
FormulaC22H19ClFN7
Cas No.1352610-25-3
SmilesCl.FC=1C=CC=CC1NCC2=NC(C3=NC(=CC=C3)C)=C(N2)C=4C=CC5=NC=NN5C4
Relative Density.no data available
Storage & Solubility Information
Storagekeep 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
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
DMSO
1mg5mg10mg50mg
50 mM0.0459 mL0.2294 mL0.4588 mL2.2942 mL
100 mM0.0229 mL0.1147 mL0.2294 mL1.1471 mL

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In Vivo Formulation Calculator (Clear solution)

Please enter your animal experiment information in the following box and click Calculate to obtain the stock solution preparation method and in vivo formula preparation method:
TargetMol | Animal experiments For example, if the intended dosage is 10 mg/kg for animals weighing 20 g , with a dosing volume of 100 μL per animal, TargetMol | Animal experiments and a total of 10 animals are to be administered, using a formulation of TargetMol | reagent 10% DMSO+ 40% PEG300+ 5% Tween 80+ 45% Saline/PBS/ddH2O , the resulting working solution concentration would be 2 mg/mL.
Stock Solution Preparation:

Dissolve 2 mg of the compound in 100 μL DMSOTargetMol | reagent 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.

Preparation of the In Vivo Formulation:

1) Add 100 μL of the DMSOTargetMol | reagent stock solution to 400 μL PEG300TargetMol | reagent 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 ddH2OTargetMol | reagent and mix thoroughly until a homogeneous solution is obtained.

This example is provided solely to demonstrate the use of the In Vivo Formulation Calculator and does not constitute a recommended formulation for any specific compound. Please select an appropriate dissolution and formulation strategy based on your experimental model and route of administration.
All co-solvents required for this protocol, includingDMSO, PEG300/PEG400, Tween 80, SBE-β-CD, and Corn oil, are available for purchase on the TargetMol website.
1 Enter information below:
mg/kg
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μL
2 Enter the in vivo formulation:
% DMSO
%
% Tween 80
% Saline/PBS/ddH2O

Dose Conversion

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Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc

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