2. Stem Cell/Wnt Apoptosis
  3. BMI1 Apoptosis
  4. PTC-028

PTC-028 est un inhibiteur du facteur de cellules souches BMI-1 dans le cancer de l’ovaire qui est oralement biodisponible. PTC-028 inhibe sélectivement les cellules cancéreuses tandis que les cellules normales qui ne sont pas affectées. PTC-028 régule à la baisse l'IMC-1, induisant l'apoptosis médiée par la caspase.

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.

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PTC-028 Chemical Structure

PTC-028 Chemical Structure

CAS No. : 1782970-28-8

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Based on 1 publication(s) in Google Scholar

PTC-028 Related Antibodies

Top Publications Citing Use of Products

1 Publications Citing Use of MCE PTC-028

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Description

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[1].

IC50 & Target

BMI-1[1]
In Vitro

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].
? 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].
? 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].
? 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].
? 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.

PTC-028 Related Antibodies

Cell Viability Assay[1]

Cell Line: OVCAR4, OV90 and CP20 cells
Concentration: 0, 25, 50, 100, 200, 500 nM
Incubation Time: 48 hours
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.

Western Blot Analysis[1]

Cell Line: OV90 and CP20 cells
Concentration: 100 nM
Incubation Time: 2, 4, 6, 12 hours
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.
In Vivo

PTC-028 (15 mg/kg; administered orally twice weekly) causes ~94% (0.169 g) reduction in tumor weight compared to the control (average tumor weight, ~3g) [1].
? 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.

Animal Model: Female athymic nude mice with implanted OV90 cells[1]
Dosage: 15 mg/kg
Administration: Orally administered; twice weekly
Result: Caused ~94% (0.169 g) reduction in tumor weight.
Animal Model: Female CD-1 mice[1]
Dosage: 10 mg/kg or 20mg/kg
Administration: Oral administered; single dose
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.
Molecular Weight

405.32

Formula

C19H12F5N5
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

FC(C1=CC=C(NC2=NC(N3C4=CC(F)=C(F)C=C4N=C3C)=CN=C2)C=C1)(F)F
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 2 years
-20°C 1 year
Solvent & Solubility
In Vitro: 

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)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.4672 mL 12.3359 mL 24.6719 mL
5 mM 0.4934 mL 2.4672 mL 4.9344 mL
View the 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.

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  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

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V2

In Vivo:

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.

  • Protocol 1

    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.
  • Protocol 2

    Add each solvent one by one:  10% DMSO    90% Corn Oil

    Solubility: ≥ 2.08 mg/mL (5.13 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator
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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Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
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.
Purity & Documentation
References

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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PTC-028 Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

PTC-0281782970-28-8PTC028PTC 028BMI1ApoptosisBmi-1B cell-specific Moloney murine leukemia virus integration site 1Inhibitorinhibitorinhibit

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