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

CI-1040 (Synonyms: PD 184352)

Cat. No.: HY-50295 Purity: 98.54%
Handling Instructions

CI-1040 (PD184352) 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 USD 66 In-stock
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50 mg USD 324 In-stock
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200 mg USD 768 In-stock
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Customer Review

Based on 9 publication(s) in Google Scholar

Top Publications Citing Use of Products

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

    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.

    CI-1040 purchased from MCE. Usage Cited in: Oncogenesis. 2019 Oct. 

    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.

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    Description

    CI-1040 (PD184352) is an orally active, highly specific, small-molecule inhibitor of MEK with an IC50 of 17 nM for MEK1.

    IC50 & Target

    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].

    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].

    Clinical Trial
    Molecular Weight

    478.66

    Formula

    C₁₇H₁₄ClF₂IN₂O₂

    CAS No.

    212631-79-3

    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 6 months
      -20°C 1 month
    Solvent & Solubility
    In Vitro: 

    DMSO : ≥ 150 mg/mL (313.37 mM)

    *"≥" 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
    10 mM 0.2089 mL 1.0446 mL 2.0892 mL
    *Please refer to the solubility information to select the appropriate solvent.
    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

    Purity: 98.54%

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