Name: 3PO
Brand: Selleck Chemicals
SKU: S7639
Availability: InStock
Rating: 5 (10 reviews)

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Quality Control

Batch: Purity: 99.94%

99.94

Related Targets	CDK HSP PD-1/PD-L1 ROCK Wee1 DNA/RNA Synthesis Microtubule Associated Ras KRas Aurora Kinase
Other PFKFB Inhibitors	PFK15 PFK158 KAN0438757

Cell Culture, Treatment & Working Concentration

Cell Lines	Assay Type	Concentration	Incubation Time	Activity Description	PMID
Jurkat	Growth inhibition assay		48 hrs	Growth inhibition of human Jurkat cells expressing inducible FLAG-tagged PFKFB incubated for 48 hrs by trypan blue dye exclusion assay, IC50=1.4μM	ChEMBL
NHBE	Growth inhibition assay		48 to 72 hrs	Growth inhibition of human NHBE cells immortalized with human telomerase and large-T antigen and transformed with mutated Ras protein incubated for 48 to 72 hrs by trypan blue dye exclusion assay, IC50=1.5μM	ChEMBL
K562	Growth inhibition assay		48 hrs	Growth inhibition of human K562 cells incubated for 48 hrs by trypan blue dye exclusion assay, IC50=3.2μM	ChEMBL
HL60	Growth inhibition assay		48 hrs	Growth inhibition of human HL60 cells incubated for 48 hrs by trypan blue dye exclusion assay, IC50=4.5μM	ChEMBL
MDA-MB-231	Growth inhibition assay		48 hrs	Growth inhibition of human MDA-MB-231 cells incubated for 48 hrs by trypan blue dye exclusion assay, IC50=4.7μM	ChEMBL
Jurkat	Growth inhibition assay		48 hrs	Growth inhibition of human Jurkat cells expressing un-altered PFKFB expression incubated for 48 hrs by trypan blue dye exclusion assay, IC50=8.9μM	ChEMBL
CRL11174	Growth inhibition assay		48 hrs	Growth inhibition of human CRL11174 cells incubated for 48 hrs by trypan blue dye exclusion assay, IC50=15μM	ChEMBL
LLC	Growth inhibition assay		48 hrs	Growth inhibition of mouse LLC cells incubated for 48 hrs by trypan blue dye exclusion assay, IC50=19μM	ChEMBL
Jurkat	Growth inhibition assay		48 hrs	Growth inhibition of human Jurkat cells expressing inducible FLAG-tagged PFKFB in presence of doxycycline incubated for 48 hrs by trypan blue dye exclusion assay, IC50=19.3μM	ChEMBL
HeLa	Growth inhibition assay		48 hrs	Growth inhibition of human HeLa cells incubated for 48 hrs by trypan blue dye exclusion assay, IC50=24μM	ChEMBL
Jurkat	Growth inhibition assay		48 hrs	Growth inhibition of PFKFB3+/-ht/LT/Ras human Jurkat cells and incubated for 48 hrs by trypan blue dye exclusion assay, IC50=26μM	ChEMBL
A549	Growth inhibition assay		48 hrs	Growth inhibition of human A549 cells incubated for 48 hrs by trypan blue dye exclusion assay, IC50=48μM	ChEMBL
Jurkat	Growth inhibition assay		48 hrs	Growth inhibition of PFKFB3+/+ht/LT/Ras human Jurkat cells and incubated for 48 hrs by trypan blue dye exclusion assay, IC50=49μM	ChEMBL
Jurkat	Cell proliferation assay	10 uM	36 hrs	Inhibition of cell proliferation of human Jurkat cells expressing inducible FLAG-tagged PFKFB at 10 uM incubated for 36 hrs by trypan blue dye exclusion assay	ChEMBL
Jurkat	Cell cycle assay			Inhibition of cell cycle arrest in human Jurkat cells expressing inducible FLAG-tagged PFKFB assessed as accumulation at G2/M phase by propidium iodide staining based flow cytometry	ChEMBL
Jurkat	Function assay	10 uM		Reduction in 2-deoxy-glucose uptake in human Jurkat cells expressing inducible FLAG-tagged PFKFB at 10 uM measured within 4 hrs using [14C]-2-deoxy-glucose by scintillation counting method	ChEMBL
Jurkat	Function assay	10 uM	4 hrs	Reduction in Fru-2,6-BP production in human Jurkat cells expressing inducible FLAG-tagged PFKFB at 10 uM measured within 4 hrs	ChEMBL
Jurkat	Function assay	10 uM	8 hrs	Reduction in lactate secretion in human Jurkat cells expressing inducible FLAG-tagged PFKFB at 10 uM after 8 hrs by lactate oxidase based colorimetric assay	ChEMBL
Jurkat	Function assay	10 uM	16 hrs	Reduction in NADH level in human Jurkat cells expressing inducible FLAG-tagged PFKFB at 10 uM after 16 hrs	ChEMBL
Jurkat	Function assay	10 uM	24 hrs	Reduction in NAD+ level in human Jurkat cells expressing inducible FLAG-tagged PFKFB at 10 uM after 24 hrs	ChEMBL
Jurkat	Function assay	10 uM	24 hrs	Reduction in ATP level in human Jurkat cells expressing inducible FLAG-tagged PFKFB at 10 uM after 24 hrs	ChEMBL
Jurkat	Function assay	10 uM	36 hrs	Suppression of glycolytic flux into lactate in human Jurkat cells expressing inducible FLAG-tagged PFKFB at 10 uM after 36 hrs by NMR spectroscopy	ChEMBL
NHBE	Growth inhibition assay	1 uM	48 to 72 hrs	Growth inhibition of human NHBE cells immortalized with human telomerase and large-T antigen and transformed with mutated Ras protein at 1 uM incubated for 48 to 72 hrs by trypan blue dye exclusion assay	ChEMBL
NHBE	Growth inhibition assay	10 uM	48 to 72 hrs	Growth inhibition of human NHBE cells immortalized with human telomerase and large-T antigen and transformed with mutated Ras protein at 10 uM incubated for 48 to 72 hrs by trypan blue dye exclusion assay	ChEMBL
Click to View More Cell Line Experimental Data

Solubility

In vitro
Batch:

DMSO : 42 mg/mL (199.78 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Ethanol : 11 mg/mL

Water : Insoluble

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
Mass value Mass unit	Concentration value Concentration unit	Volume value Volume unit	Molecular weight (g/mol)

Dilution Calculator Molecular Weight Calculator

In vivo batch selection In vivo Batch:
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	10%DMSO 1 40%PEG300 2 5%Tween80 3 45%ddH2O Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	7.000mg/ml (33.30mM)	Taking the 1 mL working solution as an example, add 100 μL of 70 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to make it clear; then continue to add 450 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

Dosage: mg/kg

Average weight of animals: g

Dosing volume per animal: μL

Number of animals:

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO

%

% Tween 80

% ddH₂O

% DMSO

+

%

Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH₂O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Chemical Information, Storage & Stability

Molecular Weight	210.23	Formula	C₁₃H₁₀N₂O	Storage (From the date of receipt)	3 years-20°Cpowder
CAS No.	18550-98-6	Download SDF		Storage of Stock Solutions	1 year-80°Cin solvent 1 month-20°Cin solvent
Synonyms	3-(3-pyridinyl)-1-(4-pyridinyl)-2-propen-1-one			Smiles	C1=CC(=CN=C1)C=CC(=O)C2=CC=NC=C2

Mechanism of Action

Targets/IC₅₀/Ki	PFKFB3 22.9 μM
In vitro	3PO is an inhibitor of the PFKFB3 isozyme primarily through competition with Fru-6-P and does not inhibit purified PFK-1 activity. This compound markedly attenuates the proliferation of several human malignant hematopoietic and adenocarcinoma cell lines (IC50, 1.4-24 μmol/L) and is selectively cytostatic to ras-transformed human bronchial epithelial cells relative to normal human bronchial epithelial cells. It can cause G2-M phase arrest.
In vivo	i.p. administration of 3PO (0.07 mg/g) to tumor-bearing mice markedly reduces the intracellular concentration of Fru-2,6-BP, glucose uptake, and growth of established tumors in vivo. It suppresses tumorigenic growth of breast adenocarcinoma, leukemia, and lung adenocarcinoma cells in vivo. The PK properties of this compound are examined in C57Bl/6 mice intravenously administered this chemical: clearance CL=2312 mL/min/kg, T_1/2=0.3 hr, C_max=113 ng/ml, AUC_0-inf=36 ng/hr/ml. It is reported to have potent activity against a highly relevant mouse model of leukemia.
References	[1] https://pubmed.ncbi.nlm.nih.gov/18202014/ [2] https://pubmed.ncbi.nlm.nih.gov/23674815/

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3PO PFKFB inhibitor

Chemical Structure

Molecular Weight: 210.23