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PTC-028

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Catalog No. T16680Cas No. 1782970-28-8

PTC-028 selectively suppresses cancer cells whereas normal cells remain unaffected. PTC-028 is an orally bioavailable inhibitor of stem cell factor BMI-1 in ovarian cancer. The depletion of BMI-1 by PTC-028 causes caspase-mediated apoptosis.

PTC-028

PTC-028

😃Good
Purity: 98.12%
Catalog No. T16680Cas No. 1782970-28-8
PTC-028 selectively suppresses cancer cells whereas normal cells remain unaffected. PTC-028 is an orally bioavailable inhibitor of stem cell factor BMI-1 in ovarian cancer. The depletion of BMI-1 by PTC-028 causes caspase-mediated apoptosis.
Pack SizePriceUSA WarehouseGlobal WarehouseQuantity
1 mg$38In StockIn Stock
2 mg$54In StockIn Stock
5 mg$89In StockIn Stock
10 mg$147In StockIn Stock
25 mg$297In StockIn Stock
50 mg$493In StockIn Stock
100 mg$723In StockIn Stock
500 mg$1,520-In Stock
1 mL x 10 mM (in DMSO)$109In StockIn Stock
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In Stock Estimated shipping dateUSA Warehouse[1-2 days] Global Warehouse[5-7 days]
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Purity:98.12%
Appearance:Solid
Color:White
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Product Introduction

Bioactivity
Description
PTC-028 selectively suppresses cancer cells whereas normal cells remain unaffected. PTC-028 is an orally bioavailable inhibitor of stem cell factor BMI-1 in ovarian cancer. The depletion of BMI-1 by PTC-028 causes caspase-mediated apoptosis.
In vitro
PTC-028 subsequently decreases BMI-1 in the biochemical functional readout. PTC-028 (100 nM; 2-12 hours) increases the phosphorylated BMI-1 species in a time-dependent manner. uH2A is observed up to 12 h with PTC-028 (100 nM) in both CP20 and OV90 cells while total H2A levels remain unchanged. PTC-028 (100 nM; 48 hours) decreases the expression of XIAP and RIPK1 while LC3B levels remain unchanged compared to that of the control. PTC-028 (25-500 nM; 48 hours) obviously reduces CP20, OVCAR4, and OV90 epithelial ovarian cancer cell 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 a minimal effect (~18-30% decrease). Significant cleavage of Caspase 7, Caspase 9, and PARP is observed in PTC-028 (100 nM; 48 hours)[1].
In vivo
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 decrease. PTC-028 (15 mg/kg; administered orally twice weekly) induces ~94% (0.169 g) reduction in tumor weight compared to the control (average tumor weight, ~3g) [1].
Chemical Properties
Molecular Weight405.32
FormulaC19H12F5N5
Cas No.1782970-28-8
SmilesCc1nc2cc(F)c(F)cc2n1-c1cncc(Nc2ccc(cc2)C(F)(F)F)n1
Relative Density.no data available
Storage & Solubility Information
StoragePowder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
Solubility Information
DMSO: 125 mg/mL (308.4 mM), Sonication is recommended.
In Vivo Formulation
10% DMSO+40% PEG300+5% Tween 80+45% Saline: 4 mg/mL (9.87 mM), Sonication is recommended.
Please add the solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately. The formulation provided above is for reference purposes only. In vivo formulations may vary and should be modified based on specific experimental conditions.
Solution Preparation Table
DMSO
1mg5mg10mg50mg
1 mM2.4672 mL12.3359 mL24.6719 mL123.3593 mL
5 mM0.4934 mL2.4672 mL4.9344 mL24.6719 mL
10 mM0.2467 mL1.2336 mL2.4672 mL12.3359 mL
20 mM0.1234 mL0.6168 mL1.2336 mL6.1680 mL
50 mM0.0493 mL0.2467 mL0.4934 mL2.4672 mL
100 mM0.0247 mL0.1234 mL0.2467 mL1.2336 mL

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Please enter your animal experiment information in the following box and click Calculate to obtain the stock solution preparation method and in vivo formula preparation method:
TargetMol | Animal experiments For example, if the intended dosage is 10 mg/kg for animals weighing 20 g , with a dosing volume of 100 μL per animal, TargetMol | Animal experiments and a total of 10 animals are to be administered, using a formulation of TargetMol | reagent 10% DMSO+ 40% PEG300+ 5% Tween 80+ 45% Saline/PBS/ddH2O , the resulting working solution concentration would be 2 mg/mL.
Stock Solution Preparation:

Dissolve 2 mg of the compound in 100 μL DMSOTargetMol | reagent to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.

Preparation of the In Vivo Formulation:

1) Add 100 μL of the DMSOTargetMol | reagent stock solution to 400 μL PEG300TargetMol | reagent and mix thoroughly until the solution becomes clear.

2) Add 50 μL Tween 80 and mix well until fully clarified.

3) Add 450 μL Saline,PBS or ddH2OTargetMol | reagent and mix thoroughly until a homogeneous solution is obtained.

This example is provided solely to demonstrate the use of the In Vivo Formulation Calculator and does not constitute a recommended formulation for any specific compound. Please select an appropriate dissolution and formulation strategy based on your experimental model and route of administration.
All co-solvents required for this protocol, includingDMSO, PEG300/PEG400, Tween 80, SBE-β-CD, and Corn oil, are available for purchase on the TargetMol website.
1 Enter information below:
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2 Enter the in vivo formulation:
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