2. MAPK/ERK Pathway Apoptosis
  3. MEK Apoptosis
  4. PD184161

PD184161 is an orally active MEK inhibitor. PD184161 inhibits MEK activity (IC50=10-100 nM) in a time- and concentration-dependent manner. PD184161 inhibits cell proliferation and induces apoptosis. PD184161 produces depressive-like behavior.

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PD184161 Chemical Structure

PD184161 Chemical Structure

CAS No. : 212631-67-9

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Based on 1 publication(s) in Google Scholar

PD184161 Related Antibodies

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Description

PD184161 is an orally active MEK inhibitor. PD184161 inhibits MEK activity (IC50=10-100 nM) in a time- and concentration-dependent manner. PD184161 inhibits cell proliferation and induces apoptosis. PD184161 produces depressive-like behavior[1][2].

IC50 & Target[1]

MEK

10-100 nM (IC50)

In Vitro

PD184161 (1-20 μM; 24, 48, or 72 hours) inhibits cell proliferation and induces apoptosis in a time and concentration dependent manner[1].
PD184161 (0.1 and 1.0 μM; 1 hour) inhibits ERK1,2 phosphorylation[1].
PD184161 (5 μM; 30 min) prevents the toxic effects of bicuculline[3].

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

PD184161 Related Antibodies

Cell Proliferation Assay[1]

Cell Line: HCC cell lines (HepG2, Hep3B, PLC, and SKHep)
Concentration: 1-20 μM
Incubation Time: 24, 48, or 72 hours
Result: Inhibited cell proliferation.

Apoptosis Analysis[1]

Cell Line: HCC cell lines (HepG2, Hep3B, PLC, and SKHep)
Concentration: 1-20 μM
Incubation Time: 48 hours
Result: Induced cell apoptosis.

Western Blot Analysis[1]

Cell Line: HCC cell lines (HepG2, Hep3B, PLC, and SKHep)
Concentration: 0.1 and 1.0 μM
Incubation Time: 1 hours
Result: Inhibited ERK1,2 phosphorylation.

Cell Viability Assay[3]

Cell Line: Primary mouse neurons
Concentration: 5 μM
Incubation Time: 30 min
Result: Prevents the toxic effects of bicuculline.
In Vivo

PD184161 reduces tumor xenograft P-ERK levels in 3-12 hours after an oral dose[1].
PD184161 (300 mg/kg; orogastric gavage twice daily for 38 days) significantly suppresses tumor engraftment and initial growth[1].
PD184161 (30 mg/kg; i.p.; single injection) produces depressive-like behavior[2].
PD184161 (500 μg/kg; intravenous injection) prevents the progression of neurological deficits and brain damage after stroke[3].

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

Animal Model: Hep3B tumor xenografts BALB/c athymic nude mice[1]
Dosage: 300 mg/kg
Administration: Orogastric gavage twice daily for 38 days
Result: Decreased the early tumor growth.
Animal Model: Male, 6 weeks C57Bl/6 mice[2]
Dosage: 500 μg/kg
Administration: intravenously in 30 min before MCAO or PTZ administration
Result: Prevented the progression of neurological deficits and brain damage after stroke.
Animal Model: C57Bl/6 mice[3]
Dosage: 30 mg/kg
Administration: i.p., single injection
Result: Produced depressive-like behavior.
Molecular Weight

557.56

Formula

C17H13BrClF2IN2O2
CAS No.
Appearance

Solid

Color

Off-white to gray

SMILES

O=C(NOCC1CC1)C2=CC(Br)=C(F)C(F)=C2NC(C(Cl)=C3)=CC=C3I
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

4°C, protect from light

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

Solvent & Solubility
In Vitro: 

DMSO : 100 mg/mL (179.35 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 1.7935 mL 8.9676 mL 17.9353 mL
5 mM 0.3587 mL 1.7935 mL 3.5871 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 (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

  • 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: 2.5 mg/mL (4.48 mM); Suspended solution; Need ultrasonic

    This protocol yields a suspended solution of 2.5 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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: ≥ 2.5 mg/mL (4.48 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 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 (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

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).

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

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 (protect from light). 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 1.7935 mL 8.9676 mL 17.9353 mL 44.8382 mL
5 mM 0.3587 mL 1.7935 mL 3.5871 mL 8.9676 mL
10 mM 0.1794 mL 0.8968 mL 1.7935 mL 4.4838 mL
15 mM 0.1196 mL 0.5978 mL 1.1957 mL 2.9892 mL
20 mM 0.0897 mL 0.4484 mL 0.8968 mL 2.2419 mL
25 mM 0.0717 mL 0.3587 mL 0.7174 mL 1.7935 mL
30 mM 0.0598 mL 0.2989 mL 0.5978 mL 1.4946 mL
40 mM 0.0448 mL 0.2242 mL 0.4484 mL 1.1210 mL
50 mM 0.0359 mL 0.1794 mL 0.3587 mL 0.8968 mL
60 mM 0.0299 mL 0.1495 mL 0.2989 mL 0.7473 mL
80 mM 0.0224 mL 0.1121 mL 0.2242 mL 0.5605 mL
100 mM 0.0179 mL 0.0897 mL 0.1794 mL 0.4484 mL
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PD184161 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:

PD184161212631-67-9PD 184161PD-184161MEKApoptosisMitogen-activated protein kinase kinaseMAPKKMAP2KHCCneuronscellstrokedepressivebehavioralcancerInhibitorinhibitorinhibit

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