PTC-028
Based on 2 publication(s) in Google Scholar
PTC-028 is an orally bioavailable inhibitor of stem cell factor BMI-1 in ovarian cancer. PTC-028 selectively inhibits cancer cells whereas normal cells remain unaffected. PTC-028 downregulates BMI-1, inducing caspase-mediated apoptosis.
Nur für Forschungszwecke. Wir verkaufen nicht an Patienten.
- Reinheit: 98.0%
- CAS. Nr.: 1782970-28-8
- Formel: C19H12F5N5
- Molecular Weight:405.32
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Speicherung:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
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Biologische Aktivität
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Chemical Information
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Lösungsmittel & Löslichkeit
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Publications Citing Use of MedChemExpress (MCE) PTC-028
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Biologische Aktivität
BMI-1[1]
PTC-028 (25-500 nM; 48 hours) significantly decreases CP20, OVCAR4 and OV90 epithelial ovarian cancer cells viability. However, in normal ovarian surface epithelial cells (OSE) and fallopian tube epithelial cells (FTE) cells, up to 500 nM treatment with PTC-028 for 48 hours has minimal effect (~18-30% decrease)[1].
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PTC-028 (100 nM; 2-12 hours) increases the phosphorylated BMI-1 species in a time-dependent manner. PTC-028 subsequently reduces BMI-1 in the biochemical functional readout [1].
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uH2A is observed up to 12 h with PTC-028 (100 nM) in both CP20 and OV90 cells while total H2A levels remain unchanged [1].
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PTC-028 (100 nM; 48 hours) decreases the expression of XIAP and RIPK1 while LC3B levels remains unchanged compared to that of the control [1].
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Significant cleavage of Caspase 7, Caspase 9 and PARP is observed in PTC-028 (100 nM; 48 hours)[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:OVCAR4, OV90 and CP20 cells
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Concentration:0, 25, 50, 100, 200, 500 nM
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Incubation Time:48 hours
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Result:OVCAR4, OV90 and CP20 cells demonstrated significant dose dependent decrease in cell viability with an IC50 of ~100 nM and ~95% decrease at 500 nM.
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Cell Line:OV90 and CP20 cells
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Concentration:100 nM
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Incubation Time:2, 4, 6, 12 hours
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Result:A time-dependent increase in the phosphorylated BMI-1 species and subsequent reduction in the biochemical functional readout.
uH2A was observed up to 12 h while total H2A levels remained unchanged.
? No obvious toxicity is noted in the animals during therapy experiments as assessed by mean body weight[1].
? PTC-028 (10 mg/kg or 20mg/kg; single oral doses) is administrated to the CD-1 mice. The Cmax is reached at both dose levels 1h post dose after which plasma concentrations slowly reduce[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Female athymic nude mice with implanted OV90 cells[1]
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Dosage:15 mg/kg
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Administration:Orally administered; twice weekly
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Result:Caused ~94% (0.169 g) reduction in tumor weight.
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Animal Model:Female CD-1 mice[1]
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Dosage:10 mg/kg or 20mg/kg
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Administration:Oral administered; single dose
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Result:Total plasma AUC0-24h were 10.9 and 26.1 μg•h/mL at doses of 10 and 20 mg/kg. The Cmax for PTC-028 at 10 and 20 mg/kg was 0.79 and 1.49 ug/mL, respectively.
Chemical Information
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CAS. Nr. 1782970-28-8
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Appearance Solid
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Molecular Weight 405.32
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Formel C19H12F5N5
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Color White to off-white
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SMILES
FC(C1=CC=C(NC2=NC(N3C4=CC(F)=C(F)C=C4N=C3C)=CN=C2)C=C1)(F)F
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (2)
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Journal Impact Factor
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Most Recent
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Cancer Cell
2025 Jun 9;43(6):1159-1174.e8. PMID: 40378837 -
Lösungsmittel & Löslichkeit
DMSO : 125 mg/mL (308.40 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.08 mg/mL (5.13 mM); Clear solution
This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Reinheit & Dokumentation
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Data Sheet (280 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
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Handling Instructions (2659 KB)
Verweise
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.4672 mL | 12.3359 mL | 24.6719 mL | 61.6797 mL |
| 5 mM | 0.4934 mL | 2.4672 mL | 4.9344 mL | 12.3359 mL | |
| 10 mM | 0.2467 mL | 1.2336 mL | 2.4672 mL | 6.1680 mL | |
| 15 mM | 0.1645 mL | 0.8224 mL | 1.6448 mL | 4.1120 mL | |
| 20 mM | 0.1234 mL | 0.6168 mL | 1.2336 mL | 3.0840 mL | |
| 25 mM | 0.0987 mL | 0.4934 mL | 0.9869 mL | 2.4672 mL | |
| 30 mM | 0.0822 mL | 0.4112 mL | 0.8224 mL | 2.0560 mL | |
| 40 mM | 0.0617 mL | 0.3084 mL | 0.6168 mL | 1.5420 mL | |
| 50 mM | 0.0493 mL | 0.2467 mL | 0.4934 mL | 1.2336 mL | |
| 60 mM | 0.0411 mL | 0.2056 mL | 0.4112 mL | 1.0280 mL | |
| 80 mM | 0.0308 mL | 0.1542 mL | 0.3084 mL | 0.7710 mL | |
| 100 mM | 0.0247 mL | 0.1234 mL | 0.2467 mL | 0.6168 mL |
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