Molecular Formula | C26H23F2N3O3
|
Molar Mass | 463.48 |
Density | 1.35 |
Melting Point | 257-259?C |
Boling Point | 801.3±65.0 °C(Predicted) |
Solubility | DMSO: soluble15mg/mL, clear |
Appearance | White solid |
Color | white to beige |
pKa | 12.76±0.20(Predicted) |
Storage Condition | -20°C |
In vitro study | YO-01027 interacts directly with the gamma-secretase complex and targets the N-terminal presenilin fragment. Administration of increasing concentrations of YO-01027 to cells expressing APPL or Notch resulted in progressive accumulation of APPL CTF fragments and complete dose-dependent reduction in NICD production. 10 μm YO-01027 reduces the number and activity of breast cancer stem cells (bcscs). A recent study showed that YO-01027 inhibited mucin MUC16 biosynthesis in undifferentiated cells before and during the fusion phase in a concentration-dependent manner via Notch inhibition, however, there is no such effect in cells at different stages after mitosis. |
In vivo study | YO-01027, intraperitoneal injection at a dose of 1 mg/ml on the day of cell injection and the following 3 days significantly reduced MCF7 tumors, but had no effect on MDA-MB-231 tumors, compared with control mice (18-28 days). It also increases the latency. YO-01027 treatment of MCF7 tumors significantly reduced tumor volume. YO-01027 treatment of C57BL/6 mice inhibited epithelial cell proliferation and dose-dependently induced goblet cell differentiation in Intestinal Adenomas. |