2. MAPK/ERK Pathway Apoptosis
  3. MEK Apoptosis
  4. Trametinib (DMSO solvate)

Trametinib (DMSO solvate)  (Synonyms: GSK-1120212 (DMSO solvate); JTP-74057 (DMSO solvate))

Cat. No.: HY-10999A Purity: 99.65%
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Trametinib (DMSO solvate) (GSK-1120212 (DMSO solvate);JTP-74057 (DMSO solvate)) is an orally active MEK inhibitor that inhibits MEK1 and MEK2 with IC50s of about 2 nM. Trametinib (DMSO solvate) activates autophagy and induces apoptosis.

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

Trametinib (DMSO solvate) Chemical Structure

Trametinib (DMSO solvate) Chemical Structure

CAS No. : 1187431-43-1

Size Price Stock Quantity
Solution
10 mM * 1 mL in DMSO USD 66 In-stock
Solid
5 mg USD 32 In-stock
10 mg USD 50 In-stock
50 mg USD 70 In-stock
100 mg USD 100 In-stock
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Customer Review

Based on 201 publication(s) in Google Scholar

Other Forms of Trametinib (DMSO solvate):

Trametinib (DMSO solvate) Related Antibodies

Top Publications Citing Use of Products

184 Publications Citing Use of MCE Trametinib (DMSO solvate)

WB

    Trametinib (DMSO solvate) purchased from MedChemExpress. Usage Cited in: Int J Cancer. 2019 Mar 15;144(6):1379-1390.  [Abstract]

    Western blot confirmed increased MAPK pathway activity in NEC-DUE2 cells when compared to NECDUE1. Treatment with PLX4032 (1 μM), GSK2118436A (100 nM), or Trametinib (100 nM) for 4 hours leads to decreased MAPK signaling in NEC-DUE2 cells. Lysates are immunoblotted for the proteins indicated.

    Trametinib (DMSO solvate) 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, Trametinib for 24 h. The levels of the total ERK was used as an input control.

    Trametinib (DMSO solvate) purchased from MedChemExpress. Usage Cited in: J Cell Sci. 2019 May 31;132(11):jcs224071.  [Abstract]

    Western blots of phosphorylated active ERK1/2 (pERK) and total ERK1/2 (ERK) for MDA MB 231 Sel2 and MDA MB 435 Sel1 populations following treatment with DMSO vehicle, 0.5 μM Trametinib or 10 μM U0126 for 18 h.

    Trametinib (DMSO solvate) purchased from MedChemExpress. Usage Cited in: Cancer Discov. 2018 Mar;8(3):354-369.  [Abstract]

    MEK inhibitor Trametinib (GSK1120212) achieves target inhibition at 3mg/kg.

    Trametinib (DMSO solvate) purchased from MedChemExpress. Usage Cited in: Sci Transl Med. 2018 Jul 18;10(450):eaaq1093.  [Abstract]

    Western blot analysis of selected MAPK and AKT/mTOR pathway components in Trametinib- and CCI-779-treated cells.

    Trametinib (DMSO solvate) purchased from MedChemExpress. Usage Cited in: J Exp Clin Cancer Res. 2018 Sep 5;37(1):218.  [Abstract]

    WB for ERRα, IDH3A, c-Myc and Cyclin D1 in the HCT116 and SW480 cells treated with the indicated concentrations of Trametinib (0-100 nM) or DMSO for 48 h.

    Trametinib (DMSO solvate) purchased from MedChemExpress. Usage Cited in: Proc Natl Acad Sci U S A. 2018 Oct 9;115(41):E9570-E9579.  [Abstract]

    presentative Western blots used to measure the efficiencies of kinase inhibitors in reducing ERK1/2 phosphorylation in control, ERK1/2 inhibitor (FR180204 and SCH772984; 10 μM)-treated or MEK1/2 inhibitor (GSK1120212; 10 μM)-treated ARPE-19 and H1299 cells.

    Trametinib (DMSO solvate) purchased from MedChemExpress. Usage Cited in: Eur J Cancer. 2018 Aug;99:37-48.  [Abstract]

    Western blot detection of cleaved PARP in H358, SW480 and HCT-116 cell lines treated with BMS-354825 (100 nM), Trametinib (400 nM) or combination for 48 h. DMSO is used as the treatment control.

    Trametinib (DMSO solvate) purchased from MedChemExpress. Usage Cited in: Biochem Biophys Res Commun. 2018 Jan 8;495(2):1846-1850.  [Abstract]

    Western blot analysis of phosphorylated ERK2, and ERK2 in microvesicle-depleted fraction (15 μg of protein) derived from viruses obtained from 10 nM Trametinib-treated CEM/LAV-1 cells.

    Trametinib (DMSO solvate) purchased from MedChemExpress. Usage Cited in: Patent. US20180161326A1.

    Trametinib (100 nM) and PLX4032 (10 μM) in combination have little effect on PARP-1 cleavage in A375 and UACC-62 cells, but significant PARP-1 cleavage and reduction in procaspase-3 level are observed via Western blot with the addition of PAC-1 (12 μM).

    Trametinib (DMSO solvate) purchased from MedChemExpress. Usage Cited in: Patent. US20180169102A1.

    The presence or absence of the pERK protein are measured through western blotting using the brain hemispheres of trametinib-administered 5×FAD mice.

    Trametinib (DMSO solvate) purchased from MedChemExpress. Usage Cited in: Sci Rep. 2017 Mar 28;7:45332.  [Abstract]

    Trametinib, a MEK1/2 inhibitor, strongly inhibits growth and partially reverses GW786034 resistance of GW786034-resistant clones.Trametinib-induced inhibition of phosphorylation of ERK1/2 in SS clones is assessed by Western blot analysis with anti-ERK1/2 and anti-phospho-ERK1/2 antibodies. SS clones are pre-treated using 10 nMtrametinib for 2 hours.

    Trametinib (DMSO solvate) purchased from MedChemExpress. Usage Cited in: Oncotarget. 2017 Feb 28;8(9):14835-14846.  [Abstract]

    MEK inhibition results in reduced ERK phosphorylation.A. Western blot analysis of SEM and KOPN8 exposed to 500 nM of MEK inhibitor or vehicle control (DMSO) for 6, 24 and 48 hours. Both cell lines almost completely lose ERK phosphorylation (p-ERK), while total ERK (t-ERK) levels remain unaffected. B. Analysis of MEK phosphorylation (p-MEK) suggests exposure to MEK162 and Selumetinib results in enhanced MEK phosphorylation in both cell lines, whereas total MEK (t-MEK) levels remain constant.

    Trametinib (DMSO solvate) purchased from MedChemExpress. Usage Cited in: Stem Cell Reports. 2016 Jan 12;6(1):74-84.  [Abstract]

    Western blot of SKPs treated with varying concentrations of Trametinib (MEKi) or DMSO (Control) for 30 min, probed for pERK1/2 and reprobed for total ERK1/2.

    Trametinib (DMSO solvate) purchased from MedChemExpress. Usage Cited in: Mol Cancer Ther. 2016 Aug;15(8):1859-69.  [Abstract]

    Addition of PAC-1 to the combination of PLX4032+Trametinib powerfully synergizes to induce apoptotic death and caspase activity in A375 and UACC-62 cells. Trametinib (100 nM) and PLX4032 (10 μM) in combination have little effect on PARP-1 cleavage in A375 and UACC-62 cells, but significant PARP-1 cleavage and reduction in procaspase-3 level are observed via Western blot with the addition of PAC-1 (12 μM).

    Trametinib (DMSO solvate) purchased from MedChemExpress. Usage Cited in: J Cell Biochem. 2016 Jun;117(6):1340-51.  [Abstract]

    HeLa S3 cells that are arrested at the G2/M border by RO-3306 treatment are washed free of RO-3306 and incubated with 10 μM GSK1120212.

    Trametinib (DMSO solvate) purchased from MedChemExpress. Usage Cited in: Cancer Discov. 2015 Sep;5(9):960-71.  [Abstract]

    The MEK inhibitor Trametinib effectively inhibits ERK phosphorylation at 30 nM in several EGFR mutant cell lines but has little effect on cell viability.

    View All MEK Isoform Specific Products:

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    MEK1 MEK2 MEK5 MEK

    • Biological Activity

    • Protocol

    • Purity & Documentation

    • References

    • Customer Review

    Description

    Trametinib (DMSO solvate) (GSK-1120212 (DMSO solvate);JTP-74057 (DMSO solvate)) is an orally active MEK inhibitor that inhibits MEK1 and MEK2 with IC50s of about 2 nM. Trametinib (DMSO solvate) activates autophagy and induces apoptosis[1][2].

    IC50 & Target[1]

    MEK1

    2 nM (IC50)

    MEK2

    2 nM (IC50)

    In Vitro

    In BRAF mutant SK-MEL-28 cells and KRAS mutant HCT116 cells, Trametinib (GSK1120212;JTP-74057) DMSO solvate causes dose-dependent inhibition of ERK1/2 phosphorylation as well as dose-dependent growth inhibition. In both SK-MEL-28 and HCT116 cells, Trametinib DMSO solvate inhibits 50% p-ERK1/2 at nearly equivalent concentrations (0.8 and 1.8 nM, respectively). However, as the slopes of the curves reflect, in SK-MEL-28 cells, Trametinib DMSO solvate inhibits 90% p-ERK1/2 at a lower concentration (3.4 nM) than in HCT116 (33.3 nM). Furthermore, in both cell lines, 50% growth inhibition is only achieved at concentrations Trametinib DMSO solvate that produces near complete ERK1/2 inhibition (85 and 90%, respectively)[2].

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

    Trametinib (DMSO solvate) Related Antibodies
    In Vivo

    Trametinib (GSK1120212;JTP-74057) is evaluated in vivo in an A549 (KRAS mutant cell line) xenograft model, orally dosing daily for 21 days (qd×21). In this study, near complete tumor growth inhibition is observed at 5.0 and 2.5 mg/kg [92 and 87% tumor growth inhibition (TGI), respectively] and to a lesser degree at 0.5 and 0.1 mg/kg (62 and 58% TGI). Although 5 mg/kg is the maximally tolerated dose (MTD) in this study, 3 mg/kg is the typically observed MTD. Dose-dependent antitumor activity with Trametinib treatment has been similarly reported for several other KRAS and BRAF mutant tumor models[2].

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

    693.53

    Formula

    C28H29FIN5O5S
    CAS No.
    Appearance

    Solid

    Color

    White to off-white

    SMILES

    CN1C(C(C)=C(N(C(N(C2=O)C3CC3)=O)C4=CC=CC(NC(C)=O)=C4)C2=C1NC5=CC=C(C=C5F)I)=O.CS(C)=O
    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 : 3.33 mg/mL (4.80 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 1.4419 mL 7.2095 mL 14.4190 mL
    5 mM --- --- ---
    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. 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)

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    Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

    This equation is commonly abbreviated as: C1V1 = C2V2

    Concentration (start)

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    Volume (start)

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    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 (3.60 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% (20% SBE-β-CD in Saline)

      Solubility: 2.5 mg/mL (3.60 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 900 μL 20% SBE-β-CD in Saline, and mix evenly.

      Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
    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: 99.65%

    COA (254 KB) LCMS (269 KB)

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

    SK-MEL-28, and HCT116 cell lines are plated in triplicate 96 well microtitre plates at 5000 cells per well in culture media. Trametinib dissolved in DMSO or negative control (0.1% DMSO) are added the following day and one plate is harvested with 50 μL of CellTiter-Glo for a time 0 (T=0) measurement. Remaining duplicate cell plates are typically incubated for 72 h. Cells are then lysed with 50 μL CellTiter-Glo, and chemiluminescent signal is read on the Wallac EnVision 2100 plate reader. For measurement of cellular ERK1/2 phosphorylation, cells are seeded and treated with Trametinib, and lysed after 72 h in Tris lysis buffer supplemented with phosphatase and protease inhibitors. All samples are analyzed with a phospho-ERK1/2 ELISA. Plates are read on MSD.SI6000 and curves are analyzed using the XLfit curve-fitting tool. For comparison of the growth assay curve and pERK1/2 assay curve, data are background subtracted and normalized to the vehicle treatment control[2].

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.
    Animal Administration
    [2]

    Mice[2]
    A549 (human non-small cell lung carcinoma) model is established from cells grown in tissue culture and harvested aseptically using a trypsin digest. Female athymic mice (strain nu/nu) are injected subcutaneously with between 5×106 and 107 cells in 50% martigel. Tumors are allowed to establish for one to four weeks before use. Trametinib is administered orally at the indicated doses in 0.2 mL/20 g by weight. Tumors are measured twice weekly using Vernier calipers. Antitumor activity is defined as tumor growth inhibition representing the % volume differential in tumor growth between the treated and control tumors at the time vehicle tumors exceeded a volume of 1000 mm3.

    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, 6 months; -20°C, 1 month. 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 1.4419 mL 7.2095 mL 14.4190 mL 36.0475 mL
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    Trametinib (DMSO solvate) 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:

    Trametinib (DMSO solvate)1187431-43-1GSK-1120212 (DMSO solvate) JTP-74057 (DMSO solvate)MEKApoptosisMitogen-activated protein kinase kinaseMAPKKMAP2KAdjuvant-inducedarthritisAIAtypeIIcollageninducedCIAorallyInhibitorinhibitorinhibit

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