2. MAPK/ERK Pathway Apoptosis
  3. MEK Apoptosis
  4. CI-1040

CI-1040 (PD 184352) is an orally active, highly specific, small-molecule inhibitor of MEK with an IC50 of 17 nM for MEK1.

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

CI-1040 Chemical Structure

CI-1040 Chemical Structure

CAS No. : 212631-79-3

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10 mM * 1 mL in DMSO
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10 mM * 1 mL in DMSO USD 67 In-stock
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10 mg USD 99 In-stock
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Customer Review

Based on 24 publication(s) in Google Scholar

CI-1040 Related Antibodies

Top Publications Citing Use of Products

    CI-1040 purchased from MedChemExpress. Usage Cited in: Biochem Pharmacol. 2023 Apr 6;211:115542.  [Abstract]

    CI-1040 (PD 184352; 10, 20, 40 nM; 48 h) significantly inhibits the expression of iNOS and COX2 in a dose-dependent manner in ATDC5 cells.

    CI-1040 purchased from MedChemExpress. Usage Cited in: Oncogenesis. 2019 Nov 4;8(11):65.  [Abstract]

    Western blot analysis of p-ERK and ERK protein levels in cell lysates of H1975 treated with AMPC, CI-1040 for 24 h. The levels of the total ERK was used as an input control.

    CI-1040 purchased from MedChemExpress. Usage Cited in: Neurotox Res. 2017 Nov;32(4):535-543.  [Abstract]

    Lithium promotes autophagy flux by activating MEK/ERK pathway in cells. Original Western blot showing LC3-II and p62 abundance following treatment with lithium in the presence of PD184352 and SCH772984 in neurons. Arithmetic means±SEM (n=5) showing LC3-II abundance following treatment with lithium in the presence of PD184352 and SCH772984 in neurons.

    View All MEK Isoform Specific Products:

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    MEK1 MEK2 MEK5 MEK

    • Biological Activity

    • Protocol

    • Purity & Documentation

    • References

    • Customer Review

    Description

    CI-1040 (PD 184352) is an orally active, highly specific, small-molecule inhibitor of MEK with an IC50 of 17 nM for MEK1.

    IC50 & Target[1]

    MEK1

    17 nM (IC50)

    In Vitro

    CI-1040 directly inhibits MEK1 with an IC50 of 17 nM. It has also been shown to have little activity against a panel of related kinases with IC50 values more than 2.5 orders of magnitude higher. Treatment of whole cells with CI-1040 completely inhibits the mitogen-stimulated phosphorylation of ERK. CI-1040 at a concentration of 1 μM is found to inhibit phosphorylation of ERK1 and ERK2 by 99% and 92%, respectively in MDA-MB-231 breast cancer cells[1]. CI-1040 induces apoptosis and inhibits proliferation in U-937 cells in a dose and time-dependent manner. CI-1040 induces a significant increase in PUMA mRNA and protein levels[2].

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

    CI-1040 Related Antibodies
    In Vivo

    The systemic administration of the MEK inhibitor CI-1040 reduces adenoma formation to a third and significantly restores lung structure. The proliferation rate of lung cells of mice treated with CL-1040 is decreased without any obvious effects on differentiation of pneumocytes[3].

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

    478.66

    Formula

    C17H14ClF2IN2O2
    CAS No.
    Appearance

    Solid

    Color

    White to off-white

    SMILES

    O=C(C1=CC=C(C(F)=C1NC2=CC=C(I)C=C2Cl)F)NOCC3CC3
    Shipping

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

    DMSO : ≥ 100 mg/mL (208.92 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 2.0892 mL 10.4458 mL 20.8917 mL
    5 mM 0.4178 mL 2.0892 mL 4.1783 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, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.

    • 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 (5.22 mM); Clear solution

      This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

      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: ≥ 2.08 mg/mL (4.35 mM); Clear solution

      This protocol yields a clear solution of ≥ 2.08 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 (20.8 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).
    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

    Purity: 99.90%

    COA (251 KB) HNMR (272 KB) LCMS (93 KB)

    Handling Instructions (2659 KB)
    References
    Cell Assay
    [2]

    The MEK inhibitor CI-1040 is dissolved in DMSO as 10 mM stock solutions and used in cell culture at final concentration 50 mg/mL. U-937 cells are pretreated for 24 hrs with 5 and 20 uM CI- 1040, then transfected with wt-p53 siRNA or PUMA siRNA for 48 hrs. Then 20 mL of MTT solution are added to each well and incubated further for 2 hours. Upon termination, the supernatant is aspirated and the MTT formazan formed by metabolically viable cells is dissolved in 100 mL of isopropanol. The plates are mixed for 30 minutes on a gyratory shaker, and absorbance is measured at 595 nm using a plate reader[2].

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.
    Animal Administration
    [3]

    Mice: The lung cancer mouse model is generated by targeting constitutively active C-Raf kinase to the lung. BAY 43-9006 or CI-1040 is daily intraperitoneal injected at a dose of 100 mg/kg from 4 months of age over a period of 21 days. Lungs were isolated and analyzed at the end of the treatment period[3].

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.
    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, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.

    Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
    DMSO 1 mM 2.0892 mL 10.4458 mL 20.8917 mL 52.2291 mL
    5 mM 0.4178 mL 2.0892 mL 4.1783 mL 10.4458 mL
    10 mM 0.2089 mL 1.0446 mL 2.0892 mL 5.2229 mL
    15 mM 0.1393 mL 0.6964 mL 1.3928 mL 3.4819 mL
    20 mM 0.1045 mL 0.5223 mL 1.0446 mL 2.6115 mL
    25 mM 0.0836 mL 0.4178 mL 0.8357 mL 2.0892 mL
    30 mM 0.0696 mL 0.3482 mL 0.6964 mL 1.7410 mL
    40 mM 0.0522 mL 0.2611 mL 0.5223 mL 1.3057 mL
    50 mM 0.0418 mL 0.2089 mL 0.4178 mL 1.0446 mL
    60 mM 0.0348 mL 0.1741 mL 0.3482 mL 0.8705 mL
    80 mM 0.0261 mL 0.1306 mL 0.2611 mL 0.6529 mL
    100 mM 0.0209 mL 0.1045 mL 0.2089 mL 0.5223 mL
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    CI-1040 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:

    CI-1040212631-79-3PD 184352CI1040CI 1040PD184352PD-184352MEKApoptosisMitogen-activated protein kinase kinaseMAPKKMAP2KInhibitorinhibitorinhibit

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