Molecular Weight(MW): 405.32
PTC-028 is an orally bioavailable compound that decreases BMI-1 levels by posttranslational modification.
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Choose Selective BMI-1 Inhibitors
|Description||PTC-028 is an orally bioavailable compound that decreases BMI-1 levels by posttranslational modification.|
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.|
|In vitro||DMSO||81 mg/mL (199.84 mM)|
|Ethanol||17 mg/mL (41.94 mM)|
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Molecular Weight Calculator
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