PTC-028

Catalog No.S8662 Batch:S866201

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Technical Data

Formula

C19H12F5N5
Molecular Weight 405.32 CAS No. 1782970-28-8
Solubility (25°C)* In vitro DMSO 81 mg/mL (199.84 mM)
Ethanol 17 mg/mL (41.94 mM)
Water Insoluble
* <1 mg/ml means slightly soluble or 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.
* Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

Preparing Stock Solutions

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 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 (from reference)

Cell Assay:

[1]
  • 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.
Animal Study:

[1]
  • Animal Models

    Preclinical model of ovarian cancer (NCr-nu mcie; 6 to 8 weeks old)

  • Dosages

    10 mg/kg and 20 mg/kg

  • Administration

    oral administration

Selleck's PTC-028 has been cited by 1 publication

Proteogenomic analysis of enriched HGSOC tumor epithelium identifies prognostic signatures and therapeutic vulnerabilities [ NPJ Precis Oncol, 2024, 8(1):68] PubMed: 38480868

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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

NOT FOR HUMAN, VETERINARY DIAGNOSTIC OR THERAPEUTIC USE.