Molecular Formula | C22H18FN7
|
Molar Mass | 399.42 |
Density | 1.40±0.1 g/cm3(Predicted) |
Melting Point | >85oC (dec.) |
Solubility | 10 mM in DMSO |
Appearance | Solid |
Color | Pale Yellow to Light Yellow |
pKa | 8.51±0.10(Predicted) |
Storage Condition | Refrigerator |
In vitro study | In HaCaT (3TP-luc) and 4T1 (3TP-luc) stable cells, 12b effectively inhibited tgf-β1-induced luciferase reporter gene activity with IC50 of 16.5 and 12.1 nM, respectively. EW-7197 inhibited TGFβ-induced phosphorylation of Smad2 or Smad3 and epithelial-to-mesenchymal transformation (EMT) in TGFβ-treated breast cancer cells. In addition, EW-7197 also abrogated tgfβ1-induced tumor cell migration and invasion in mammary gland cells. |
In vivo study | In rats, EW-7197 has an oral bioavailability of 51% with a high systemic exposure dose (AUC) of 1426 ng × h/mL and a maximum plasma concentration (Cmax). 1620 ng/mL. EW-7197 also exhibit low toxicity to the cardiovascular system, central nervous system, and respiratory system. In the mouse B16 melanoma model, EW-7197 (2.5 mg/kg daily, p.o.) enhanced cytotoxic T-lymphocyte (CTL) responses and inhibited melanoma growth. EW-7197 enhanced the activity of cytotoxic T lymphocytes in 4T1 orthotopic transplanted mice and increased the survival time of 4T1-Luc and 4T1 mammary tumor mice. |