1. TGF-beta/Smad
  2. TGF-β Receptor

Vactosertib Hydrochloride (Synonyms: EW-7197 (Hydrochloride); TEW-7197 (Hydrochloride))

Cat. No.: HY-19928A Purity: 98.57%
Handling Instructions

Vactosertib Hydrochloride (EW-7197 Hydrochloride) is a small-molecule ATP-competitive inhibitor of TGFβRI (ALK5) with an IC50 of 12.9 nM.

For research use only. We do not sell to patients.

Vactosertib Hydrochloride Chemical Structure

Vactosertib Hydrochloride Chemical Structure

CAS No. : 1352610-25-3

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10 mM * 1 mL in DMSO USD 125 In-stock
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Other Forms of Vactosertib Hydrochloride:

  • Biological Activity

  • Protocol

  • Technical Information

  • Purity & Documentation

  • References

Description

Vactosertib Hydrochloride (EW-7197 Hydrochloride) is a small-molecule ATP-competitive inhibitor of TGFβRI (ALK5) with an IC50 of 12.9 nM.

IC50 & 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].

Clinical Trial
Solvent & Solubility
In Vitro: 

DMSO : 50 mg/mL (114.71 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.2942 mL 11.4710 mL 22.9421 mL
5 mM 0.4588 mL 2.2942 mL 4.5884 mL
10 mM 0.2294 mL 1.1471 mL 2.2942 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.5 mg/mL (5.74 mM); Clear solution

  • 2.

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.5 mg/mL (5.74 mM); Clear solution

  • 3.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 2.5 mg/mL (5.74 mM); Clear solution

References
Cell Assay
[2]

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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Administration
[1]

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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

References
Molecular Weight

435.88

Formula

C₂₂H₁₉ClFN₇

CAS No.

1352610-25-3

SMILES

CC1=CC=CC(C2=C(C3=CN4C(C=C3)=NC=N4)NC(CNC5=CC=CC=C5F)=N2)=N1.Cl

Storage

-20°C, stored under nitrogen

Shipping

Room temperature in continental US; may vary elsewhere

Purity: 98.57%

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Product Name:
Vactosertib Hydrochloride
Cat. No.:
HY-19928A
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Vactosertib Hydrochloride

Cat. No.: HY-19928A