Vactosertib Hydrochloride

SKU: orb1707320

Description

Vactosertib Hydrochloride (EW-7197 Hydrochloride) is an orally bioavailable, ATP-competitive inhibitor of ALK5 (TGF-β receptor I). It demonstrates anti-metastatic and anticancer activity in vitro and in vivo, and research shows it can sensitize pancreatic cancer cells to gemcitabine by inhibiting cell viability.

Research Area

Cardiovascular Research, Signal Transduction, Stem Cell & Developmental Biology

Key Properties

• CAS Number: 1352610-25-3
• MW: 435.89
• Purity: 98.03%
• Formula: C₂₂H₁₉ClFN₇
• SMILES: Cl.FC=1C=CC=CC1NCC2=NC(C3=NC(=CC=C3)C)=C(N2)C=4C=CC5=NC=NN5C4
• Target: TGF-beta/Smad,ALK
• Solubility: 10% DMSO+40% PEG300+5% Tween 80+45% Saline:4 mg/mL (9.18 mM);H2O:20 mg/mL (45.88 mM);DMSO:100 mg/mL (229.42 mM)

Bioactivity

• Target IC50:
  ALK2/4:17.3 nM|ALK5:12.9 nM
• 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.
• 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).

Storage & Handling

• Storage: keep 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.
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

EW7197 Hydrochloride, EW-7197 Hydrochloride, EW 7197 Hydrochloride, NOV 1301 Hydrochloride, NOV1301 Hydrochloride, ALK5, Vactosertib Hydrochloride, TEW 7197 Hydrochloride, TEW7197 Hydrochloride, TEW-7197 Hydrochloride

Compound Identifiers

PubChem CID

54766014