PD 184161 |
Catalog No.GC15646
One-Click Copy Product Info
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MEK1/2 inhibitor
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 212631-67-9
Sample solution is provided at 25 µL, 10mM.
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IC50: 10-100 nM
PD 184161 is a MEK1/2 inhibitor.
The intracellular signaling pathway of mitogen-activated protein kinases is involved in the regulation of various cellular functions. One of these pathways, named Raf/MEK/ERK pathway, plays a key role in the regulation of cellular differentiation, growth, and proliferation. The modulation of this Raf/MEK/ERK pathway has been reported as a useful approach to treate proliferative disorders such as cancer.
In vitro: Previous study found that PD184161 could inhibit MEK activity in a time- and concentration-dependent manner, which was more effectively than PD098059 or U0126. Moreover, PD184161 could inhibit cell proliferation and induce apoptosis at concentrations of > or = 1.0 μM time- and concentration-dependently [1].
In vivo: Animal study showd that tumor xenograft P-ERK levels were significantly reduced 3 to 12 hours after an oral dose of PD184161. Contrarily, tumor xenograft P-ERK levels following long-term treatment of PD184161 were refractory to this signaling effect. PD184161 also significantly suppressed tumor engraftment and initial growth, however, established tumors were not significantly affected. In summary, PD184161 has antitumor effects in HCC in vivo that appear to correlate with suppression of MEK activity [1].
Clinical trial: So far, no clinical study has been conducted.
Reference:
[1] Klein, P. J.,Schmidt, C.M.,Wiesenauer, C.A., et al. The effects of a novel MEK inhibitor PD184161 on MEK-ERK signaling and growth in human liver cancer. Neoplasia 8(1), 1-8 (2006).
| Cas No. | 212631-67-9 | SDF | |
| Chemical Name | 5-bromo-2-[(2-chloro-4-iodophenyl)amino]-N-(cyclopropylmethoxy)-3,4-difluoro-benzamide | ||
| Canonical SMILES | FC1=C(NC2=C(Cl)C=C(I)C=C2)C(C(NOCC3CC3)=O)=CC(Br)=C1F | ||
| Formula | C17H13BrClF2IN2O2 | M.Wt | 557.6 |
| Solubility | ≤10mg/ml in ethanol;30mg/ml in DMSO;30mg/ml in dimethyl formamide | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
||
| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
|
1 mg | 5 mg | 10 mg |
| 1 mM | 1.7934 mL | 8.967 mL | 17.934 mL |
| 5 mM | 358.7 μL | 1.7934 mL | 3.5868 mL |
| 10 mM | 179.3 μL | 896.7 μL | 1.7934 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)
Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )
Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL saline, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
- Purity: >98.00% Appearance: A solid
- COA (Certificate of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 2 reference(s) in Google Scholar.)