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3PO

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Catalog No. T22223Cas No. 18550-98-6

3PO is a small-molecule inhibitor of PFKFB3 (IC50: 22.9 μM), inhibiting the proliferation of several human malignant hematopoietic and adenocarcinoma cell lines (IC50: 1.4-24 μM). It suppresses glucose uptake, and decreases the intracellular concentration of Fru-2,6-BP, lactate, ATP, NAD+, and NADH.

3PO

3PO

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Purity: 99.67%
Catalog No. T22223Cas No. 18550-98-6
3PO is a small-molecule inhibitor of PFKFB3 (IC50: 22.9 μM), inhibiting the proliferation of several human malignant hematopoietic and adenocarcinoma cell lines (IC50: 1.4-24 μM). It suppresses glucose uptake, and decreases the intracellular concentration of Fru-2,6-BP, lactate, ATP, NAD+, and NADH.
Pack SizePriceUSA WarehouseGlobal WarehouseQuantity
5 mg$52In StockIn Stock
10 mg$74In StockIn Stock
25 mg$129In StockIn Stock
50 mg$198In StockIn Stock
100 mg$358-In Stock
200 mg$533-In Stock
500 mg$849-In Stock
1 mL x 10 mM (in DMSO)$58In 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:99.67%
Appearance:Solid
Color:White
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Product Introduction

Bioactivity
Description
3PO is a small-molecule inhibitor of PFKFB3 (IC50: 22.9 μM), inhibiting the proliferation of several human malignant hematopoietic and adenocarcinoma cell lines (IC50: 1.4-24 μM). It suppresses glucose uptake, and decreases the intracellular concentration of Fru-2,6-BP, lactate, ATP, NAD+, and NADH.
Targets&IC50
PFKFB3:22.9 μM
In vitro
3PO markedly attenuates the proliferation of several human malignant hematopoietic and adenocarcinoma cell lines (IC50, 1.4-24 μM) and is selectively cytostatic to ras-transformed human bronchial epithelial cells relative to normal human bronchial epithelial cells. Compared with the wild-type PFKFB3+/+transformed cells (IC50, 49 μM), the PFKFB3+/- fibroblasts were more sensitive to compound 3PO treatment (IC50, 26 μM). 3PO Causes G2-M phase arrest, which Is preceded by decreased Fru-2,6-BP and glucose uptake. 3PO slows growth through inhibition of PFK-2 activity, then ectopic expression of the PFKFB3 isozyme may thwart the cytostatic activity of 3PO. [1] 3PO inhibits the glycolytic regulator PFKFB3 in endothelial cells (ECs). 3PO decreases glycolysis in ECs and impairs vessel sprouting. 3PO also suppresses vascular hyperbranching induced by inhibition of Notch or VEGF receptor 1 (VEGFR1) and amplified the antiangiogenic effect of VEGF blockade[2].
In vivo
Compared with vehicle control, compound 3PO treatment significantly reduced Fru-2,6-BP in tumor xenografts (vehicle: 13.1 ± 1.9 pmol/mg, 3PO: 8.5 ± 1.7 pmol/mg). [1] 3PO also impairs (pathological) angiogenesis.
Chemical Properties
Molecular Weight210.23
FormulaC13H10N2O
Cas No.18550-98-6
SmilesO=C(\C=C\c1cccnc1)c1ccncc1
Relative Density.1.192 g/cm3 (Predicted)
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
H2O: Insoluble
DMSO: 40 mg/mL (190.27 mM), Sonication is recommended.
Ethanol: 11 mg/mL (52.32 mM), Sonication is recommended.
In Vivo Formulation
10% DMSO+40% PEG300+5% Tween 80+45% Saline: 2.5 mg/mL (11.89 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
Ethanol/DMSO
1mg5mg10mg50mg
1 mM4.7567 mL23.7835 mL47.5670 mL237.8348 mL
5 mM0.9513 mL4.7567 mL9.5134 mL47.5670 mL
10 mM0.4757 mL2.3783 mL4.7567 mL23.7835 mL
20 mM0.2378 mL1.1892 mL2.3783 mL11.8917 mL
50 mM0.0951 mL0.4757 mL0.9513 mL4.7567 mL
DMSO
1mg5mg10mg50mg
100 mM0.0476 mL0.2378 mL0.4757 mL2.3783 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:
% DMSO
%
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