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PFK158 PFKFB inhibitor

Name: PFK158
Brand: Selleck Chemicals
SKU: S8807
Availability: InStock
Rating: 5 (8 reviews)

Cat.No.S8807

PFK158 is a potent and selective inhibitor of PFKFB3. It has improved PK properties and causes ~80% growth inhibition in several mouse models of human-derived tumors.

Chemical Structure

Molecular Weight: 328.29

Jump to Mechanism of Action Solubility Chemical Information, Storage & Stability Specificity

Quality Control

Batch: Purity: 99.22%

99.22

Related Targets	DNA/RNA Synthesis CDK Microtubule Associated Ras HSP PD-1/PD-L1 Aurora Kinase Casein Kinase Rho Serine/threonin kinase eIF Chk ROCK Myc Kinesin PLK DHFR PAK PERK DYRK RUNX PP2A AP-1 MPS1 Wee1 p21 BMI-1 LIM kinase Nur77 APC
Related Products	PFK15 3PO KAN0438757 PFKFB3 Antibody [M5H12] PFKFB3 Antibody [A21K14] PFKP Antibody [E13C9] PFKFB2 Antibody [P13H13] Phospho-PFKFB2 (Ser483) Antibody [A5G21] PFKM Antibody [F13D16]

Chemical Information, Storage & Stability

Molecular Weight	328.29	Formula	C₁₈H₁₁F₃N₂O	Storage (From the date of receipt)	3 years -20°C powder
CAS No.	1462249-75-7	--		Storage of Stock Solutions	1 year-80°Cin solvent 1 month-20°Cin solvent
Synonyms	N/A			Smiles	C1=CC(=CC2=C1C=CC(=N2)C=CC(=O)C3=CC=NC=C3)C(F)(F)F

Solubility

In vitro
Batch:

DMSO : 14 mg/mL (42.64 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Ethanol : 4 mg/mL

Water : Insoluble

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
=	×	×

Dilution Calculator Molecular Weight Calculator

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.
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.
Clear solution	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	3.300mg/ml (10.05mM)	Taking the 1 mL working solution as an example, add 50 μL of 66 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 clarify; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.
Clear solution	5% DMSO 1 95% Corn oil Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	3.300mg/ml (10.05mM)	Taking the 1 mL working solution as an example, add 50 μL of 66 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results.

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.

Mechanism of Action

Targets/IC₅₀/Ki	PFKFB3 ^[1]
In vitro	PFK158 results in reduced glucose uptake, ATP production, lactate release as well as induction of apoptosis in gynecologic cancer cells. This compound treatment sensitizes chemoresistant cells and induces cell death^[1].
References	[1] https://pubmed.ncbi.nlm.nih.gov/30226266/

Tech Support

Handling Instructions

Tel: +1-832-582-8158 Ext:3

If you have any other enquiries, please leave a message.

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