2. MAPK/ERK Pathway
  3. MEK
  4. PD318088

PD318088 is a potent, allosteric and non-ATP competitive MEK1/2 inhibitor, an analog of PD184352 (HY-50295). PD318088 binds simultaneously with ATP in a region of the MEK1 active site that is adjacent to the ATP-binding site. PD318088 can be used for cancer research.

For research use only. We do not sell to patients.

PD318088 Chemical Structure

PD318088 Chemical Structure

CAS No. : 391210-00-7

Size Price Stock Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 165 In-stock
Solution
10 mM * 1 mL in DMSO USD 165 In-stock
Solid
5 mg USD 134 In-stock
10 mg USD 206 In-stock
25 mg USD 433 In-stock
50 mg USD 654 In-stock
100 mg USD 988 In-stock
200 mg   Get quote  
500 mg   Get quote  

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Customer Review

Based on 1 publication(s) in Google Scholar

PD318088 Related Antibodies

Top Publications Citing Use of Products

1 Publications Citing Use of MCE PD318088

View All MEK Isoform Specific Products:

View All Isoforms
MEK1 MEK2 MEK5 MEK

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

PD318088 is a potent, allosteric and non-ATP competitive MEK1/2 inhibitor, an analog of PD184352 (HY-50295). PD318088 binds simultaneously with ATP in a region of the MEK1 active site that is adjacent to the ATP-binding site. PD318088 can be used for cancer research[1].

IC50 & Target[1][2]

MEK1

 

MEK2

 

In Vitro

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[1].
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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

PD318088 Related Antibodies
Molecular Weight

561.09

Formula

C16H13BrF3IN2O4
CAS No.
Appearance

Solid

Color

Light yellow to yellow

SMILES

BrC1=CC(C(NOCC(CO)O)=O)=C(C(F)=C1F)NC2=CC=C(C=C2F)I
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 2 years
-20°C 1 year
Solvent & Solubility
In Vitro: 

DMSO : ≥ 100 mg/mL (178.22 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.7822 mL 8.9112 mL 17.8225 mL
5 mM 0.3564 mL 1.7822 mL 3.5645 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

  • Molarity Calculator

  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass
=
Concentration
×
Volume
×
Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 2.75 mg/mL (4.90 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.75 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (27.5 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
  • Protocol 2

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in Saline)

    Solubility: ≥ 2.75 mg/mL (4.90 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.75 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (27.5 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

    Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 1.7822 mL 8.9112 mL 17.8225 mL 44.5561 mL
5 mM 0.3564 mL 1.7822 mL 3.5645 mL 8.9112 mL
10 mM 0.1782 mL 0.8911 mL 1.7822 mL 4.4556 mL
15 mM 0.1188 mL 0.5941 mL 1.1882 mL 2.9704 mL
20 mM 0.0891 mL 0.4456 mL 0.8911 mL 2.2278 mL
25 mM 0.0713 mL 0.3564 mL 0.7129 mL 1.7822 mL
30 mM 0.0594 mL 0.2970 mL 0.5941 mL 1.4852 mL
40 mM 0.0446 mL 0.2228 mL 0.4456 mL 1.1139 mL
50 mM 0.0356 mL 0.1782 mL 0.3564 mL 0.8911 mL
60 mM 0.0297 mL 0.1485 mL 0.2970 mL 0.7426 mL
80 mM 0.0223 mL 0.1114 mL 0.2228 mL 0.5570 mL
100 mM 0.0178 mL 0.0891 mL 0.1782 mL 0.4456 mL
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PD318088 Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

PD318088391210-00-7PD 318088PD-318088MEKMitogen-activated protein kinase kinaseMAPKKMAP2KInhibitorinhibitorinhibit

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