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 | |
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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 | |
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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 |
Species | Mouse | Rat | Rabbit | Guinea pig | Hamster | Dog |
Weight (kg) | 0.02 | 0.15 | 1.8 | 0.4 | 0.08 | 10 |
Body Surface Area (m2) | 0.007 | 0.025 | 0.15 | 0.05 | 0.02 | 0.5 |
Km factor | 3 | 6 | 12 | 8 | 5 | 20 |
Animal A (mg/kg) = Animal B (mg/kg) multiplied by | Animal B Km |
Animal A Km |
For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.
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