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PF-9366

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Catalog No. T5191Cas No. 72882-78-1

PF-9366 is a human methionine adenosyltransferase 2A (Mat2A) inhibitor with an IC50 of 420 nM and a Kd of 170 nM.

PF-9366

PF-9366

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Purity: 99.88%
Catalog No. T5191Cas No. 72882-78-1
PF-9366 is a human methionine adenosyltransferase 2A (Mat2A) inhibitor with an IC50 of 420 nM and a Kd of 170 nM.
Pack SizePriceUSA WarehouseGlobal WarehouseQuantity
1 mg$40In StockIn Stock
5 mg$93In StockIn Stock
10 mg$139In StockIn Stock
25 mg$253In StockIn Stock
50 mg$357In StockIn Stock
100 mg$490In StockIn Stock
200 mg$713In StockIn Stock
1 mL x 10 mM (in DMSO)$98In StockIn Stock
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In Stock Estimated shipping dateUSA Warehouse[1-2 days] Global Warehouse[5-7 days]
This molecule is a custom-made product. TargetMol has an excellent synthesis team with the experience and capability to provide you with cost-effective products.If you have any questions, please feel free to contact us. We are committed to serving you wholeheartedly.
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Purity:99.88%
Appearance:Solid
Color:White
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Product Introduction

Bioactivity
Description
PF-9366 is a human methionine adenosyltransferase 2A (Mat2A) inhibitor with an IC50 of 420 nM and a Kd of 170 nM.
Targets&IC50
Mat2A:420 nM (cell free)
In vitro
H520 lung carcinoma cells were treated with PF-9366 for 6 h. PF-9366 inhibited cellular SAM production with an IC50 of 1.2 μM. The IC50s of PF-9366 was modestly decreased in the H520 cells with Mat2B knockdown, to 0.86 mM. Huh-7 cells were more sensitive to compound exposure than the H520 cell line. After 6-h exposure to PF-9366, the IC50 for SAM synthesis inhibition was 225 nM.
Kinase Assay
The Mat2A and Mat2B proteins are extensively dialyzed into a buffer containing 150 mM KCl, 25 mM HEPES, pH 7.4, 5 mM MgCl2, 5% (v/v) glycerol, 2 mM TCEP. Concentrations are determined spectrophotometrically using an ?280 of 44,350 /M.cm for Mat2A and an ?280 of 36,440 /M.cm for Mat2B. PF-9366 are diluted from 100% DMSO stocks into a buffer without DMSO. In a typical experiment, nineteen 15 μL injections of 200 μM compound or 30-35 μM Mat2B are made into 10 μM Mat2A on a VP ITC or nineteen 2 μL injections of 200 μM compound into 10 μM Mat2A on an Auto iTC200.
Cell Research
Huh-7 cells are seeded at a concentration of 15,000 cells per well for 6-h incubation with compound (PF-9366) and 4,000 cells per well for 72-h incubation with the compound in 96-well plates in 200 μL of growth medium. NCI-H520 MAT2B knockdown cells are seeded at a concentration of 20,000 cells per well for 6 h incubation or 10,000 cells per well for 72 h incubation with the compound in 96 well plates in 200 μL of growth medium. Cells are allowed to attach overnight at 37°C with 5% CO2. A 5× solution of cycloleucine is prepared fresh from powder stock in the growth medium. Other compounds (PF-9366) are diluted in 100% DMSO using a three-fold dilution scheme and further diluted in growth medium to give 0.5% DMSO final. Consistency of cellular confluence for each cell line is monitored with the IncuCyte Zoom live cell imager. Proliferation is measured using CellTiterGlo reagent. Growth media is removed from the cell plates following compound treatment and 80 μL/well CellTiter Glo diluted 1:1 in PBS added.
Chemical Properties
Molecular Weight350.84
FormulaC20H19ClN4
Cas No.72882-78-1
SmilesCN(C)CCc1nnc2cc(-c3ccccc3)c3cc(Cl)ccc3n12
Relative Density.1.25 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
DMSO: 20 mg/mL (57.01 mM), Sonication is recommended.
In Vivo Formulation
10% DMSO+40% PEG300+5% Tween 80+45% Saline: 2 mg/mL (5.7 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 mM2.8503 mL14.2515 mL28.5030 mL142.5151 mL
5 mM0.5701 mL2.8503 mL5.7006 mL28.5030 mL
10 mM0.2850 mL1.4252 mL2.8503 mL14.2515 mL
20 mM0.1425 mL0.7126 mL1.4252 mL7.1258 mL
50 mM0.0570 mL0.2850 mL0.5701 mL2.8503 mL

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In Vivo Formulation Calculator (Clear solution)

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:
mg/kg
g
μL
2 Enter the in vivo formulation:
% DMSO
%
% Tween 80
% Saline/PBS/ddH2O

Dose Conversion

You can also refer to dose conversion for different animals. More Dose Conversion

Tech Support

Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc

Keywords

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