PTC-028

Catalog No.S8662

PTC-028 Chemical Structure

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

Biological Activity

Description PTC-028 is an orally bioavailable compound that decreases BMI-1 levels by posttranslational modification.
Targets
BMI-1 [1]
()
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[1].

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[1].

Protocol

Cell Research:

[1]

+ Expand
  • Cell lines: Immortalized ovarian surface epithelium (OSE) or the fallopian tube epithelium(FTE) cells and ovarian cancer cells
  • Concentrations: 0-500 nmol/L
  • Incubation Time: 48 h
  • Method:

    Cells are treated with PTC-028 at the indicated concentrations for 48 hours and cellular viability is assessed using the MTS assay.


    (Only for Reference)
Animal Research:

[1]

+ Expand
  • 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
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 81 mg/mL (199.84 mM)
Ethanol 17 mg/mL (41.94 mM)
Water Insoluble

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 405.32
Formula

C19H12F5N5

CAS No. 1782970-28-8
Storage powder
in solvent
Synonyms N/A

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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID