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In vitro: SH5-07 blocks STAT3 DNA binding activity in vitro and in human glioma, breast, and prostate cancer cells and in v-Src-transformed murine fibroblasts. STAT3-dependent gene transcription is blocked along with Bcl-2, Bcl-xL, Mcl-1, Cyclin D1, c-Myc and Survivin expression. In vivo: In mouse xenograft models of glioma and breast cancer, administration of SH5-07 effectively inhibits tumor growth.
| Cell Experiment | |
|---|---|
| Cell lines | Normal mouse fibroblasts (NIH3T3) |
| Preparation method | Cells are treated with 0-8 μM agent for 24-48 h. For cell cycle profile analysis, cells are harvested and fixed with 70% ice-cold ethanol and stained with propidium iodide (PI). For apoptosis analysis, cells are collected and stained with FITC-Annexin V using Apoptosis Detection Kit. Both the DNA content of cells and the Annexin V-positive cells are analyzed by FACScan flow cytometer. Cell cycle phase distribution is analyzed using the Cell-Fit program. Data acquisition is gated to exclude cell doublets. |
| Concentrations | 0-8 μM |
| Incubation time | 24-48 h |
| Animal Experiment | |
|---|---|
| Animal models | female athymic nude mice |
| Formulation | 1% DMSO |
| Dosages | 3, 5 or 6 mg/kg |
| Administration | oral gavage/tail vein injection |
| Molecular Weight | 625.61 |
| Formula | C29H28F5N3O5S |
| CAS Number | 1456632-41-9 |
| Solubility (25°C) | DMSO 50 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
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