PD184161
Based on 2 publication(s) in Google Scholar
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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- Pureté : 99.01%
- CAS No.: 212631-67-9
- Formule: C17H13BrClF2IN2O2
- Masse moléculaire:557.56
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Stockage:
4°C, protect from light
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Activité biologique
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Chemical Information
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Solvant et solubilité
- Protocole
- Pureté et documentation
- Références
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Help & FAQs
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Publications Citing Use of MedChemExpress (MCE) PD184161
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Activité biologique
Description
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.
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Cell Line:HCC cell lines (HepG2, Hep3B, PLC, and SKHep)
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Concentration:1-20 μM
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Incubation Time:24, 48, or 72 hours
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Result:Inhibited cell proliferation.
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Cell Line:HCC cell lines (HepG2, Hep3B, PLC, and SKHep)
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Concentration:1-20 μM
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Incubation Time:48 hours
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Result:Induced cell apoptosis.
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Cell Line:HCC cell lines (HepG2, Hep3B, PLC, and SKHep)
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Concentration:0.1 and 1.0 μM
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Incubation Time:1 hours
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Result:Inhibited ERK1,2 phosphorylation.
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Cell Line:Primary mouse neurons
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Concentration:5 μM
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Incubation Time:30 min
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Result:Prevents the toxic effects of bicuculline.
In Vivo
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.
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Animal Model:Hep3B tumor xenografts BALB/c athymic nude mice[1]
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Dosage:300 mg/kg
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Administration:Orogastric gavage twice daily for 38 days
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Result:Decreased the early tumor growth.
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Animal Model:Male, 6 weeks C57Bl/6 mice[2]
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Dosage:500 μg/kg
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Administration:intravenously in 30 min before MCAO or PTZ administration
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Result:Prevented the progression of neurological deficits and brain damage after stroke.
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Animal Model:C57Bl/6 mice[3]
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Dosage:30 mg/kg
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Administration:i.p., single injection
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Result:Produced depressive-like behavior.
- Annexin V plus membrane-impermeant dye apoptosis staining
- BrdU Incorporation Assay
- Somatic Cell Culture
- Protocol for Tail Suspension Test (TST)
- CFSE Dye Dilution Proliferation Assay
- Dye-dilution cell tracking and proliferation staining
- CCK-8/WST-8 Cell Proliferation Assay
- Protocol for Cell Cycle
- Cell Counting-Based Growth Curve Assay
- Colony Formation (Clonogenic) Assay
- Cell Viability Determination by MTT Colorimetric Assay
- EdU Incorporation Assay (Click Chemistry-Based DNA Synthesis Measurement)
- Ki-67 Immunostaining Proliferation Assay
- Detection of Apoptosis
- TUNEL staining for apoptotic DNA fragmentation
- PCNA Immunodetection Proliferation Assay
- Protocol for Cell Counting and Cell Density Analysis
- Apoptosis Solutions
- MTT Cell Proliferation Assay
- Protocol for Forced Swim Test (FST)
- Protocol for Sucrose Preference Test (SPT)
Chemical Information
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CAS No. 212631-67-9
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Appearance Solid
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Masse moléculaire 557.56
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Formule C17H13BrClF2IN2O2
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Color Off-white to gray
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SMILES
O=C(NOCC1CC1)C2=CC(Br)=C(F)C(F)=C2NC(C(Cl)=C3)=CC=C3I
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
4°C, protect from light
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
Publications (2)
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Journal Impact Factor
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Most Recent
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Cell
2024 Feb 1;187(3):609-623.e21. PMID: 38244548 -
Anal Chem
Exposome-Scale Investigation of Cl-/Br-Containing Chemicals Using High-Resolution Mass Spectrometry, Multistage Machine Learning, and Cloud Computing. [Abstract]2025 Jun 3;97(21):11099-11109. PMID: 40401576
Solvant et solubilité
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)
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.
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.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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.
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.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
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).
Working solution concentration: 0.22 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)
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
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.
Pureté et documentation
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Fiche technique (280 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
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Instruction de manipulation (2659 KB)
Références
[1]. Klein PJ, et al. The effects of a novel MEK inhibitor PD184161 on MEK-ERK signaling and growth in human liver cancer. Neoplasia. 2006 Jan;8(1):1-8. [Content Brief]
[2]. Duman CH, et al. A role for MAP kinase signaling in behavioral models of depression and antidepressant treatment. Biol Psychiatry. 2007 Mar 1;61(5):661-70. [Content Brief]
[3]. Gladbach A, et al. ERK inhibition with PD184161 mitigates brain damage in a mouse model of stroke. J Neural Transm (Vienna). 2014 May;121(5):543-7. [Content Brief]
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 |
PD184161 Related Classifications
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