1. MAPK/ERK Pathway
  2. MEK
  3. Trametinib DMSO solvate

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

Cat. No.: HY-10999A Purity: 99.77%
Handling Instructions

Trametinib DMSO solvate is a potent MEK inhibitor that specifically inhibits MEK1/2, with an IC50 value of about 2 nM.

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

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10 mM * 1 mL in DMSO USD 66 In-stock
Estimated Time of Arrival: December 31
10 mg USD 60 In-stock
Estimated Time of Arrival: December 31
50 mg USD 96 In-stock
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100 mg USD 143 In-stock
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Customer Review

Based on 65 publication(s) in Google Scholar

Other Forms of Trametinib DMSO solvate:

Top Publications Citing Use of Products

Publications Citing Use of MCE Trametinib DMSO solvate

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

    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 MCE. Usage Cited in: Cancer Discov. 2015 Sep;5(9):960-71.

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

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

    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 MCE. Usage Cited in: Cancer Discov. 2018 Mar;8(3):354-369.

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

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

    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 MCE. Usage Cited in: Mol Cancer Ther. 2016 Aug;15(8):1859-69.

    Addition of PAC-1 to the combination of Vemurafenib+Trametinib powerfully synergizes to induce apoptotic death and caspase activity in A375 and UACC-62 cells. Trametinib (100 nM) and Vemurafenib (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 MCE. Usage Cited in: Oncotarget. 2017 Feb 28;8(9):14835-14846.

    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 MCE. Usage Cited in: Sci Rep. 2017 Mar 28;7:45332.

    Trametinib, a MEK1/2 inhibitor, strongly inhibits growth and partially reverses Pazopanib resistance of Pazopanib-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 MCE. Usage Cited in: Patent. US20180161326A1.

    Trametinib (100 nM) and Vemurafenib (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 MCE. Usage Cited in: Eur J Cancer. 2018 Aug;99:37-48.

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

    Trametinib DMSO solvate purchased from MCE. 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 MCE. Usage Cited in: Sci Transl Med. 2018 Jul 18;10(450). pii: eaaq1093.

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

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

    Western blot confirmed increased MAPK pathway activity in NEC-DUE2 cells when compared to NECDUE1. Treatment with Vemurafenib (1 μM), Dabrafenib (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 MCE. Usage Cited in: J Exp Clin Cancer Res. 2018 Sep 5;37(1):218.

    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 MCE. Usage Cited in: Proc Natl Acad Sci U S A. 2018 Oct 9;115(41):E9570-E9579.

    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 MCE. Usage Cited in: Sci Signal. 2018 Oct 30;11(554). pii: eaar6795. 

    MEK1 mutants with in-frame deletions of the β3-αC loop exhibit differential resistance to MEK inhibitors (Trametinib, GDC0623, cobimetinib, AZD6244, and binimentinib).

    Trametinib DMSO solvate purchased from MCE. Usage Cited in: J Cell Sci. 2019 May 31;132(11). pii: jcs224071. 

    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.

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    Description

    Trametinib DMSO solvate is a potent MEK inhibitor that specifically inhibits MEK1/2, with an IC50 value of about 2 nM.

    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) 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].

    In Vivo

    Trametinib (GSK1120212) DMSO solvate 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 DMSO solvate treatment has been similarly reported for several other KRAS and BRAF mutant tumor models[2].

    Clinical Trial
    Molecular Weight

    693.53

    Formula

    C₂₈H₂₉FIN₅O₅S

    CAS No.

    1187431-43-1

    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 : 69 mg/mL (99.49 mM; Need ultrasonic)

    H2O : < 0.1 mg/mL (insoluble)

    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 0.2884 mL 1.4419 mL 2.8838 mL
    10 mM 0.1442 mL 0.7209 mL 1.4419 mL
    *Please refer to the solubility information to select the appropriate solvent.
    In Vivo:
    • 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

    • 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

    • 3.

      Add each solvent one by one:  10% DMSO    90% corn oil

      Solubility: ≥ 2.5 mg/mL (3.60 mM); Clear solution

    *All of the co-solvents are provided by MCE.
    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

    Purity: 99.77%

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    Trametinib DMSO solvate
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