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Trametinib

(Synonyms: GSK1120212; JTP-74057)
300 Cited Publications
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Based on 300 publication(s) in Google Scholar

Trametinib (GSK1120212; JTP-74057) is an orally active MEK inhibitor that inhibits MEK1 and MEK2 with IC50s of about 2 nM. Trametinib activates autophagy and induces apoptosis, cross the blood-brain barrier (BBB), used in research related to subarachnoid hemorrhage (SAH).

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  • Pureza: 99.93%
  • No. CAS: 871700-17-3
  • Fòrmula: C26H23FIN5O4
  • Peso molecular:615.39
  • Almacenamiento:
    Powder   -20°C, 3 years , 4°C, 2 years ; In solvent   -80°C, 6 months , -20°C, 1 month
  • Trametinib Chemical Structure
    Trametinib Chemical Structure
  • Experimental Validation Results for Trametinib
  • Experimental Validation Results for Trametinib
  • Experimental Validation Results for Trametinib
  • Experimental Validation Results for Trametinib
  • Experimental Validation Results for Trametinib
  • Experimental Validation Results for Trametinib
  • Experimental Validation Results for Trametinib
  • Experimental Validation Results for Trametinib
  • Experimental Validation Results for Trametinib
  • Experimental Validation Results for Trametinib
  • Experimental Validation Results for Trametinib
  • Experimental Validation Results for Trametinib
  • Experimental Validation Results for Trametinib
  • Experimental Validation Results for Trametinib
  • Experimental Validation Results for Trametinib
  • Experimental Validation Results for Trametinib
  • Experimental Validation Results for Trametinib
  • Experimental Validation Results for Trametinib
  • Experimental Validation Results for Trametinib
  • Experimental Validation Results for Trametinib
  • Experimental Validation Results for Trametinib
No. CAS: 871700-17-3
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  • Trametinib Chemical Structure
    Trametinib Chemical Structure
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    Trametinib purchased from MedChemExpress. Usage Cited in: Mol Cancer. 2024 Sep 20;23(1):204. [Abstract]

    Customer Validation
     Trametinib (0.1 µM; 24-96 h) significantly suppresses the proliferation of EG cells derived from FL (fetal liver) and CB (cord blood), with stronger inhibition observed when used in combination with Venetoclax (0.1 µM; 24-96 h).

  • 1/16

    Trametinib purchased from MedChemExpress. Usage Cited in: Mol Cancer. 2023 May 20;22(1):86. [Abstract]

    Customer Validation
     Western blot of PITPNC1 expression in A549, H2009 and HPAFII cells treated for 24 h with pharmacologic inhibitors: trametinib (MEKi, 0.5 μmol/L), BIX02189 (MEK5i, 10 μmol/L), SP600125 (JNKi, 10 μmol/L) or GSK2126458 (PI3Ki, 0.1 μmol/L). Twenty μg of protein were loaded per sample. β-TUBULIN was used as loading marker. I Western blot of PITPNC1 and KRAS expression in Kraslox/lox MEFs transduced with different human HA-tagged KRAS mutants (G12C, G12D, G12V, G12R, G12S, G13D and Q61H)

  • 1/16

    Trametinib purchased from MedChemExpress. Usage Cited in: Mil Med Res. 2023 Dec 20;10(1):68. [Abstract]

    Customer Validation
     After treatment with pharmacological inhibitors of PI3K (GDC-0326, 1 μmol/L), MEK (trametinib, 100 nmol/L), or mTOR (everolimus, 100 nmol/L); a PI3K inhibitor combined with an mTOR inhibitor; or an MEK inhibitor combined with an mTOR inhibitor for 48 h, KLC primary cells were lysed to extract total proteins. Thereafter, Western blotting was employed to measure the protein levels of p-mTOR, p-S6, p-4EBP1, p-70S6K, p-Akt and p-ERK.

  • 1/16

    Trametinib purchased from MedChemExpress. Usage Cited in: Cancer Cell. 2020 Mar 16;37(3):387-402.e7. [Abstract]

    Customer Validation
     MCF-7 cells were seeded in 10-11 M E2 to which fulvestrant (F), dabrafenib (D), trametinib (T) or selumetinib (S) were subsequently added at 10-9, 10-6, 10-7 or 10-6 M, respectively. After 6 days, proteins were measured by immunoblotting, and phosphorylation levels (as defined by the levels of the phosphorylated form over total protein) relative to the vehicle-treated cells were set to 1.

  • 1/16

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

    Customer Validation
     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.

  • 1/16

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

    Customer Validation
     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.

  • 1/16

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

    Customer Validation
     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.

  • 1/16

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

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

  • 1/16

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

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

  • 1/16

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

    Customer Validation
     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.

  • 1/16

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

    Customer Validation
     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.

  • 1/16

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

    Customer Validation
     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.

  • 1/16

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

    Customer Validation
     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.

  • 1/16

    Trametinib purchased from MedChemExpress. Usage Cited in: Patent. US20180161326A1.

    Customer Validation
     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).

  • 1/16

    Trametinib purchased from MedChemExpress. Usage Cited in: Patent. US20180169102A1.

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

  • 1/16

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

    Customer Validation
     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.

  • 1/16

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

    Customer Validation
     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.

  • 1/16

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

    Customer Validation
     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).

  • 1/16

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

    Customer Validation
     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.

  • 1/16

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

    Customer Validation
     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.

  • 1/16

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

    Customer Validation
     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