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PD318088

Name: PD318088
Brand: TargetMol
SKU: T6152
Price: 43 USD
Availability: InStock
Rating: 5 (10 reviews)

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Catalog No. T6152Cas No. 391210-00-7

PD318088 is a non-ATP competitive allosteric MEK1/2 inhibitor, binding simultaneously with ATP in a region of the MEK1 active site that is adjacent to the ATP-binding site.

PD318088

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Purity: 99.60%

Catalog No. T6152Cas No. 391210-00-7

PD318088 is a non-ATP competitive allosteric MEK1/2 inhibitor, binding simultaneously with ATP in a region of the MEK1 active site that is adjacent to the ATP-binding site.

Pack Size	Price	USA Warehouse	Global Warehouse
1 mg	$43	In Stock	In Stock
5 mg	$109	In Stock	In Stock
10 mg	$169	In Stock	In Stock
25 mg	$357	In Stock	In Stock
50 mg	$539	In Stock	In Stock
100 mg	$818	-	In Stock
1 mL x 10 mM (in DMSO)	$135	In Stock	In Stock

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In Stock Estimated shipping dateUSA Warehouse[1-2 days] Global Warehouse[5-7 days]

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Batch Information

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Purity:99.60%

Appearance:Solid

Color:Yellow

Resource Download

COA HNMR LCMS

Product Introduction

Bioactivity

Description	PD318088 is a non-ATP competitive allosteric MEK1/2 inhibitor, binding simultaneously with ATP in a region of the MEK1 active site that is adjacent to the ATP-binding site.
In vitro	PD318088 is a small-molecule inhibitor of MEK1/2, which is an analog of PD184352, suggesting it might have substantial anti-proliferative activity against cancer cells, although no functional study of PD318088 is currently available. PD318088 binds simultaneously with ATP in a region of the MEK1 active site that is adjacent to the ATP-binding site. Formation of the ternary complexes with PD318088 and MgATP results in moderate increases (to 140 nM) for the Kd monomer-dimer for both MEK1 and MEK2. The binding of PD318088 and MgATP to MEK1 also abolishes the formation of tetramers and higher-order aggregates. PD318088 and MgATP together increase the dimerization disassociation constant for MEK1 and MEK2 slightly from ~75 nM to ~140 nM, suggesting that the mechanism of inhibition for PD318088 is probably a result of localized conformational changes in the active site and not a global change in the overall structure. [1]
Kinase Assay	Enzyme Assays: Phosphatidylinositide 3-kinase inhibitory activity was determined using a scintillation proximity assay in the presence of 1 μmol/L ATP. Inhibition of mTOR protein kinase was determined using a TR-FRET-based LanthaScreen method from Invitrogen. Compounds were assayed at a maximum concentration of 10 μmol/L in the presence of 1 μmol/L ATP, and IC50 values were determined using GraphPad Prism software.

Chemical Properties

Molecular Weight	561.09
Formula	C₁₆H₁₃BrF₃IN₂O₄
Cas No.	391210-00-7
Smiles	OCC(O)CONC(=O)c1cc(Br)c(F)c(F)c1Nc1ccc(I)cc1F
Relative Density.	1.993 g/cm3

Storage & Solubility Information

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.

Solubility Information

Ethanol: 14 mg/mL (24.95 mM), Sonication is recommended.

H2O: < 1 mg/mL (insoluble or slightly soluble)

DMSO: 112 mg/mL (199.61 mM), Sonication is recommended.

In Vivo Formulation

10% DMSO+40% PEG300+5% Tween 80+45% Saline: 4 mg/mL (7.13 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

	1mg	5mg	10mg	50mg
1 mM	1.7822 mL	8.9112 mL	17.8225 mL	89.1123 mL
5 mM	0.3564 mL	1.7822 mL	3.5645 mL	17.8225 mL
10 mM	0.1782 mL	0.8911 mL	1.7822 mL	8.9112 mL
20 mM	0.0891 mL	0.4456 mL	0.8911 mL	4.4556 mL

DMSO

	1mg	5mg	10mg	50mg
50 mM	0.0356 mL	0.1782 mL	0.3564 mL	1.7822 mL
100 mM	0.0178 mL	0.0891 mL	0.1782 mL	0.8911 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:

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 DMSO TargetMol | 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 DMSO TargetMol | reagent stock solution to 400 μL PEG300 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 ddH₂O TargetMol | 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.

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