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GSK1120212 (Trametinib)

Cat. No. M1759

All AbMole products are for research use only, cannot be used for human consumption.

GSK1120212 (Trametinib) Structure
Synonym:

JTP-74057, GSK212

Size Price Availability Quantity
Free Sample (0.5-1 mg)  USD 0 In stock
10mM*1mL in DMSO USD 35  USD35 In stock
5mg USD 20  USD20 In stock
10mg USD 30  USD30 In stock
50mg USD 70  USD70 In stock
100mg USD 110  USD110 In stock
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Biological Activity

Trametinib (GSK1120212;  Jtp-74057) is an orally effective MEK inhibitor with IC50 of 2 nM against MEK1 and MEK2, respectively. Trametinib can activate autophagy and induce apoptosis.

Product Citations
Customer Product Validations & Biological Datas
Source Cancer Cell (2018). Figure 5. Trametinib (Abmole Bioscience, Houston, USA)
Method oral gavage
Cell Lines Mice
Concentrations 0.1 mg/kg
Incubation Time —
Results Mice treated with IRN + VCR had stable disease (SD), whereas mice treated with either palbociclib + trametinib or abemaciclib + trametinib exhibited progressive disease.
Source Int J Mol Sci (2018). Figure 5. GSK1120212 (AbMole BioScience, Houston, TX, USA)
Method vitro experiments
Cell Lines CAR-T cells
Concentrations 30 nM
Incubation Time 16 h
Results CAR-T cells in the conditions without inhibitor, with DMSO solvent control, with Vem alone, Tram alone, Dabra alone, and the combination Dabra + Tram
Source Int J Mol Sci (2018). Figure 4. GSK1120212 (AbMole BioScience, Houston, TX, USA)
Method vitro experiments
Cell Lines CAR-T cells
Concentrations 30 nM
Incubation Time 16 h
Results The presence of Vem alone, Tram alone,Cobi alone, Vem + Cobi, and Dabra + Tram, but not of Dabra alone seemed to reduce these quantities to approximately 50%.
Source Int J Mol Sci (2018). Figure 3. GSK1120212 (AbMole BioScience, Houston, TX, USA)
Method vitro experiments
Cell Lines CAR-T cells
Concentrations 30 nM
Incubation Time 16 h
Results The condition with Vem + Cobi was similarly inhibited as Vem alone, while the Dabra + Tram condition was significantly less inhibited
Source Int J Mol Sci (2018). Figure 2. GSK1120212 (AbMole BioScience, Houston, TX, USA)
Method vitro experiments
Cell Lines CAR-T cells
Concentrations 30 nM
Incubation Time 16 h
Results Incubation with the MEK inhibitors Tram and Cobi alone, but also the combination of Vem + Cobi reduced the CD25 upregulation approximately to 50%
Source Biochem Pharmacol (2015). GSK1120212, Figure 5. (Abmole Bioscience Kowloon, Hong Kong, China)
Method western blot
Cell Lines CD4+ T cells
Concentrations 20 mM
Incubation Time 24 h
Results Addition of GSK1120212, an inhibitor of MEK to the growth media diminished phosphorylation of ERK, but showed no noticeable effect on the inhibition of arctigenin against mTORC1 activation (Fig. 5D).
Source J Bio Chem (2014). Figure 9. GSK1120212 (AbMole BioScience).
Method Rats in the inhibitor groups were treated with GSK1120212
Cell Lines
Concentrations 0.3 mg/kg
Incubation Time
Results In animals receiving GSK1120212, shockwave treatment did not significantly change the percentage of Ki-67 or phospho-Erk1/2 positive cells (Figure 9B and C). These data support our findings that ischemic wound healing in shockwave treated animals is significantly enhanced by shockwave treatment and is dependent on Erk1/2 pathways.
Source J Bio Chem (2014). Figure 8. GSK1120212 (AbMole BioScience).
Method Rats in the inhibitor groups were treated with GSK1120212
Cell Lines
Concentrations
Incubation Time
Results "Planimetric analysis of the wound size area on the ischemic side of the epigastric flap was performed immediately after surgery (day 0) and on days 1, 5, and 10 after surgery (Figure 8C and D) Shockwave treatment of the ischemic side of the epigastric flap (100 pulses at 0.13 mJ/mm2) significantly decreased the wound size compared to control animals (Figure 8A). In animals receiving the Mek1/2 inhibitor GSK1120212 (0.1 mg/kg daily), wound sizes in the control and shockwave groups did not differ (Figure 8B). These results suggest that shockwave treatment exerts its beneficial effects on wound healing by induction of Erk1/2 signaling."
Source Biochemical Pharmacology (2015). Figure 7. LY294002, MK-2206 and GSK1120212 were gifts from Abmole Bioscience (Kowloon, Hong Kong).
Method Western blot
Cell Lines Purified CD4+ T cells
Concentrations 20 mM LY294002, 10 mM MK-2206 as well as 10 mM GSK1120212
Incubation Time 3 h
Results Arctigenin could inhibit mTORC1 activation via a way independent of PI3K/AKT and ERK.
Source J. Biol. Chem (2015). Figure 1. GSK1120212 (AbMole BioScience)
Method IHC
Cell Lines none
Concentrations 0.1 mg/kg daily
Incubation Time 10 days
Results Ischemic wound healing in shockwave treated animals is significantly enhanced by shockwave treatment and is dependent on Erk1/2 pathways.
Source J. Biol. Chem (2015). Figure 8. GSK1120212 (AbMole BioScience)
Method shockwave treatment in vivo
Cell Lines control
Concentrations 0.1 mg/kg daily
Incubation Time 10 days
Results Shockwave treatment enhances wound healing in a rat model by promoting proliferation via Erk1/2 signaling
Protocol (for reference only)
Cell Experiment
Cell lines DO4, MM415, MM485, SK-MEL-2, MaMel30I and MaMel27II
Preparation method cells were plated in 96-well plates with a density of 4000-8000 cells per well and incubated for 24 h at 37 °C with 5% C02. Then cells were incubated with increasing drug concentrations and their combinations. Cell viability was measured with the CellTiter-Glo (CTG) Luminescent Cell Viability Assay (Promega; Madison, Wisconsin, USA) according to the manufacturer’s protocol. Luminescence was measured on the SynergyHT plate reader (BioTek, Vermont, USA) using Gen5 software (Version 1.11.5). For apoptotic assays, cells were plated in 12-well plates and treated with DMSO, trametinib, metformin or combinations. After 72hrs apoptosis was assessed using the Dead Cell Apoptosis Kit with Annexin V Alexa Fluor 488 & Propidium Iodide according to the manufacturer’s protocol (Invitrogen; V13241) with the AccuriC6 Flow Cytometer using the CFlow software (Version 1.0.227.4).
Concentrations 0.2-30nM
Incubation time 72 h
Animal Experiment
Animal models Tumor induction on the skin of the Tyr::CreERT2; PtenLoxP/LoxP;BrafCA/+ mice
Formulation dissolved in 0.5% hydroxypropyl methylcellulose (Sigma-Aldrich) and 0.2% Tween-80 (Sigma-Aldrich)
Dosages 0.75 mg/kg, once daily
Administration orally
Chemical Information
Molecular Weight 615.39
Formula C26H23FIN5O4
CAS Number 871700-17-3
Solubility (25°C) DMSO 30 mg/mL
Storage Powder          -20°C   3 years ;  4°C   2 years
In solvent       -80°C   6 months ;  -20°C   1 month
References

[1] Khalili JS et al. Clin Cancer Res. Combination Small Molecule MEK and PI3K Inhibition Enhances Uveal Melanoma Cell Death in a Mutant GNAQ- and GNA11-Dependent Manner.

[2] Jing J et al. Mol Cancer Ther. Comprehensive predictive biomarker analysis for MEK inhibitor GSK1120212.

[3] Yamaguchi T et al. Int J Oncol. Antitumor activities of JTP-74057 (GSK1120212), a novel MEK1/2 inhibitor, on colorectal cancer cell lines in vitro and in vivo.

[4] Gilmartin AG et al. Clin Cancer Res. GSK1120212 (JTP-74057) is an inhibitor of MEK activity and activation with favorable pharmacokinetic properties for sustained in vivo pathway inhibition.

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Keywords: GSK1120212 (Trametinib), JTP-74057, GSK212 supplier, MEK, inhibitors, activators

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