2. MAPK/ERK Pathway
  3. MEK
  4. PD 198306

PD 198306 is a selective MAPK/ERK-kinase (MEK) inhibitor. PD 198306 results in an observable reduction in the Streptozocin induced increase in the level of active ERK1 and 2. Antihyperalgesic effects.

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PD 198306 Chemical Structure

PD 198306 Chemical Structure

CAS No. : 212631-61-3

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10 mM * 1 mL in DMSO
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Based on 1 publication(s) in Google Scholar

PD 198306 Related Antibodies

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Description

PD 198306 is a selective MAPK/ERK-kinase (MEK) inhibitor. PD 198306 results in an observable reduction in the Streptozocin induced increase in the level of active ERK1 and 2. Antihyperalgesic effects[1].

IC50 & Target[1]

MEK

 

In Vitro

PD198306 significantly inhibits Tha-GFP replication by 25% at 10 μM, after 36 h[2].
PD198306 (5 μM) reduces Tha-Crimson replication significantly by 20% at 18 h but such a result could not be confirmed at 36 h[2].

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

PD 198306 Related Antibodies

Cell Cycle Analysis[2]

Cell Line: Human induced pluripotent stem cells (iPSC)
Concentration: 10  μM
Incubation Time: 6  hours
Result: Inhibited Tha-Crimson replication at 10 μM, reducing it by 30% at 18 h and 50% at 36 h.
In Vivo

Intrathecal administration of PD 198306 (1-30 μg per 10 μL) dose-dependently (1-30 μg) blocks static allodynia in both the streptozocin and the chronic constriction injury (CCI) models of neuropathic pain[1].

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

Animal Model: Male Sprague Dawley rats (250-300 g) bearing neuropathic pain[1]
Dosage: 1-30 μg per 10 μL and 3 mg per 100 μL (PD 198306 is suspended in cremophor:ethanol:water, 1 : 1 : 8.)
Administration: Single doses of intrathecal (i.t.) or intraplantar (ipl) of PD 198306 (1-30 μg per 10 μL and 3 mg per 100 μL respectively
Result: Intrathecal administration dose-dependently (1-30 μg) blocked static allodynia the streptozocin model of neuropathic pain.
The minimum effective doses (MED) of 3 μg significantly blocked static allodynia 30 min after treatment.
Both 10 μg and the highest dose used (30 μg) totally blocked the maintenance of static allodynia, for up to 1 h.
Molecular Weight

476.23

Formula

C18H16F3IN2O2
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

O=C(NOCC1CC1)C(C=C(F)C(F)=C2F)=C2NC3=C(C=C(I)C=C3)C
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 200 mg/mL (419.97 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.0998 mL 10.4991 mL 20.9983 mL
5 mM 0.4200 mL 2.0998 mL 4.1997 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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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  • Dilution Calculator

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

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

This equation is commonly abbreviated as: C1V1 = C2V2

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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: ≥ 5 mg/mL (10.50 mM); Clear solution

    This protocol yields a clear solution of ≥ 5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 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% Corn Oil

    Solubility: ≥ 5 mg/mL (10.50 mM); Clear solution

    This protocol yields a clear solution of ≥ 5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

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mg/kg

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g

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(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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.0998 mL 10.4991 mL 20.9983 mL 52.4956 mL
5 mM 0.4200 mL 2.0998 mL 4.1997 mL 10.4991 mL
10 mM 0.2100 mL 1.0499 mL 2.0998 mL 5.2496 mL
15 mM 0.1400 mL 0.6999 mL 1.3999 mL 3.4997 mL
20 mM 0.1050 mL 0.5250 mL 1.0499 mL 2.6248 mL
25 mM 0.0840 mL 0.4200 mL 0.8399 mL 2.0998 mL
30 mM 0.0700 mL 0.3500 mL 0.6999 mL 1.7499 mL
40 mM 0.0525 mL 0.2625 mL 0.5250 mL 1.3124 mL
50 mM 0.0420 mL 0.2100 mL 0.4200 mL 1.0499 mL
60 mM 0.0350 mL 0.1750 mL 0.3500 mL 0.8749 mL
80 mM 0.0262 mL 0.1312 mL 0.2625 mL 0.6562 mL
100 mM 0.0210 mL 0.1050 mL 0.2100 mL 0.5250 mL
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PD 198306 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:

PD 198306212631-61-3PD198306PD-198306MEKMitogen-activated protein kinase kinaseMAPKKMAP2KRNAinterferencedrugscreeninginositolphosphatephosphatasesmitogen-activated proteinkinasesrabiesMAPKERKantihyperalgesicneuropathicpainInhibitorinhibitorinhibit

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