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PTC-028 is an orally bioavailable inhibitor of stem cell factor BMI-1, it downregulates BMI-1, inducing caspase-mediated apoptosis. PTC-028 is an orally bioavailable compound that decreases BMI-1 levels by posttranslational modification.
In vitro: PTC-028 is an orally bioavailable compound that decreases BMI-1 levels by posttranslational modification. PTC-028 treatment selectively inhibits cancer cells in clonal growth and viability assays, whereas normal cells remain unaffected. Hyperphosphorylation-mediated depletion of cellular BMI-1 by PTC-028 coupled with a concurrent temporal decrease in ATP and a compromised mitochondrial redox balance potentiates caspase-dependent apoptosis.
In vivo: In vivo, orally administered PTC-028, as a single agent, exhibits significant antitumor activity comparable with the standard cisplatin/paclitaxel therapy in an orthotopic mouse model of ovarian cancer. After administration of single oral doses to the CD-1 mice, total plasma AUC0-24h are 10.9 and 26.1 mg/h/mL at doses of 10 and 20 mg/kg, showing dose proportional pharmacokinetics. The Cmax for PTC-028 at 10 and 20 mg/kg is 0.79 and 1.49 mg/mL, respectively. The Cmax is reached at both dose levels 1-hour postdose after which plasma concentrations slowly reduce.
| Cell Experiment | |
|---|---|
| Cell lines | Immortalized ovarian surface epithelium (OSE) or the fallopian tube epithelium(FTE) cells and ovarian cancer cells |
| Preparation method | Cells are treated with PTC-028 at the indicated concentrations for 48 hours and cellular viability is assessed using the MTS assay. |
| Concentrations | 0-500 nmol/L |
| Incubation time | 48 h |
| Animal Experiment | |
|---|---|
| Animal models | Preclinical model of ovarian cancer (NCr-nu mcie; 6 to 8 weeks old) |
| Formulation | 0.5% HPMC,1% Tween 80 |
| Dosages | 10 mg/kg and 20 mg/kg |
| Administration | oral administration |
| Molecular Weight | 405.32 |
| Formula | C19H12F5N5 |
| CAS Number | 1782970-28-8 |
| Form | Solid |
| Solubility (25°C) | DMSO 90 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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