Vactosertib

SKU: orb1300718

Description

Vactosertib (EW-7197) is an orally active, small-molecule inhibitor targeting the TGF-β receptor type I (ALK5). It is widely used in cancer research to investigate TGF-β signaling pathways in both in vitro cellular assays and in vivo animal models for its potential antitumor effects.

Research Area

Cardiovascular Research, Signal Transduction, Stem Cell & Developmental Biology

Key Properties

• CAS Number: 1352608-82-2
• MW: 399.42
• Purity: 99.81% (May vary between batches)
• Formula: C₂₂H₁₈FN₇
• SMILES: Cc1cccc(n1)-c1[nH]c(CNc2ccccc2F)nc1-c1ccc2ncnn2c1
• Target: ALK,TGF-beta/Smad
• Solubility: DMSO:252.5 mg/mL (632.17 mM);Ethanol:40 mg/mL (100.15 mM);H2O:< 1 mg/mL (insoluble or slightly soluble)

Bioactivity

• Target IC50:
  ALK4:13 nM|ALK5:11 nM
• In Vivo:
  In rats, Vactosertib shows an oral bioavailability of 51% with high systemic exposure (AUC) of 1426 ng×h/mL and maximum plasma concentration (Cmax) of 1620 ng/mL. Vactosertib also shows low toxicity on the cardiovascular system, central nervous system, and respiratory system. In a mouse B16 melanoma model, Vactosertib (2.5 mg/kg daily p.o.) suppresses the progression of melanoma with enhanced cytotoxic T-lymphocyte (CTL) responses. 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.
• In Vitro:
  In HaCaT (3TP-luc) and 4T1 (3TP-luc) stable cells, 12b potently inhibits the TGF-β1-induced luciferase reporter activity with IC50 of 16.5 and 12.1 nM, respectively. Vactosertib inhibits TGFβ-induced Smad2 or Smad3 phosphorylation and the epithelial-to-mesenchymal transition (EMT) in TGFβ-treated breast cancer cells. In addition, Vactosertib also abrogates TGFβ1-induced tumor cell migration and invasion in breast cells.
• Cell Research:
  Cells are seeded in 96 well plate and treated with indicated concentrations of EW-7197 in 0.2% HI-FBS medium for 72 h. Cells are dried after incubation with 10% TCA in media. Then, cells are incubated with 0.4% SRB (Sulforhodamine B) in 1% acetic acid for 30 min. After washing with 1% glacial acetic acid, bounded dye is released in 10 mM Tris buffer (pH 10.5) for 30 min. Absorbance is measured at 570 nm. (Only for Reference)

Storage & Handling

• Storage: Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

Vactosertib, Transforming growth factor beta receptors, Smad, TEW 7197, TEW7197, TEW-7197, TGF-b/Smad, TGFbeta, TGFb, TGF-β Receptor, TGF-β/Smad, TGFβ, TGF-beta, TGFbeta/Smad, survival, p38α, Inhibitor, EW7197, EW-7197, EW 7197, inhibit, invasion, migration, antimetastatic, cancer, ALK5, ALK3, ALK4, ALK2, ALK1, breast, cell

Compound Identifiers

PubChem CID

54766013