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Trametinib

Trametinib
Trametinib (GSK1120212) is a MEK inhibitor that inhibits MEK1 and MEK2 (IC50=0.7/0.9 nM) with ATP non-competitive and oral activity. Trametinib activates autophagy and induces apoptosis.
Catalog No. T2125Cas No. 871700-17-3
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Purity:99.88%
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Trametinib

Catalog No. T2125Cas No. 871700-17-3

Trametinib (GSK1120212) is a MEK inhibitor that inhibits MEK1 and MEK2 (IC50=0.7/0.9 nM) with ATP non-competitive and oral activity. Trametinib activates autophagy and induces apoptosis.
All TargetMol products are for research purposes only and cannot be used for human consumption. We do not provide products or services to individuals. Please comply with the intended use and do not use TargetMol products for any other purpose.
Pack SizePriceAvailabilityQuantity
5 mg$24.8$31In Stock
10 mg$40$50In Stock
50 mg$51.2$64In Stock
100 mg$80$100In Stock
200 mg$112.8$141In Stock
1 mL x 10 mM (in DMSO)$40$50In Stock
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Product Introduction

Bioactivity
Description
Trametinib (GSK1120212) is a MEK inhibitor that inhibits MEK1 and MEK2 (IC50=0.7/0.9 nM) with ATP non-competitive and oral activity. Trametinib activates autophagy and induces apoptosis.
Targets&IC50
MEK2:0.92 nM (cell free), MEK1:1.8 nM (cell free)
In vitro
METHODS: Mouse intrahepatic cholangiocarcinoma cells SB1, LD-1 and human intrahepatic cholangiocarcinoma cells EGI-1 were treated with Trametinib (0-10,000 nM) for 48 h, and cell growth inhibition was detected by MTT.
RESULTS: Trametinib dose-dependently inhibited the growth of SB1, LD-1 and EGI-1 cells with IC50 of 41.48 nM, 56.10 nM and 27.89 nM, respectively. [1]
METHODS: Human colon cancer cells RKO were treated with Trametinib (200 nmol/L) for 30 h. The expression levels of target proteins were detected by Western Blot.
RESULTS: Trametinib significantly reduced the levels of p-ERK and p-AKT. [2]
METHODS: Human glioma cells U87 and U251 were incubated with Trametinib (50 nM) for 6-72 h. Apoptosis was detected by Flow Cytometry.
RESULTS: Trametinib induced a significant increase in apoptosis in U87 and U251 cells, and Trametinib induced late apoptosis but not early apoptosis in glioma cells. [3]
In vivo
METHODS: To detect anti-tumor activity in vivo, Trametinib (0.3-1 mg/kg) was orally administered to BALB/c-nu/nu mice bearing human colorectal cancer tumors HT-29 and COLO205 once daily for fourteen days.
RESULTS: Trametinib treatment significantly inhibited the growth of human colorectal cancer tumors, indicating antitumor activity in vivo. [4]
METHODS: To assay antitumor activity in vivo, Trametinib (5 mg/kg) was injected intraperitoneally three times a week for fourteen days into NSG mice bearing human B-lymphoblastic leukemia tumors KOPN8 and COLO205.
RESULTS: Trametinib monotherapy delayed the progression of leukemia, but was not sufficient to prevent leukemia growth. [5]
Kinase Assay
A Raf-MEK-ERK cascade kinase assay was carried out as previously described. Briefly, nonphosphorylated myelin basic protein (MBP) was coated onto an ELISA plate, and the active form of B-Raf/c-Raf was mixed with unphosphorylated MEK1/MEK2 and ERK2 in 10 μM ATP and 12.5 mM MgCl2 containing MOPS buffer in the presence of various concentrations of JTP-74057. The phosphorylation of MBP was detected by the anti-phosphoMBP antibody. Kinase inhibitory activities against a total of 99 kinases were tested by kinase profiler at 10 μM ATP [1].
Cell Research
These cells were maintained in media recommended by the providers. Exponentially growing cells were precultured in 96-well tissue culture plates for 24 h and then exposed to JTP-74057. Cell growth was determined by an in vitro toxicology assay kit, sulforhodamine B based. For combination studies, two compounds were simultaneously added to the HT-29 cells and incubated for 72 h. In the presence of various concentrations of compound A, the 50% inhibitory concentration (IC50) values of compound B were determined. Then, the fixed concentration of compound A versus the IC50 value of compound B was plotted. Conversely, the IC50 values of compound A were determined in the presence of various concentrations of compound B and plotted [1].
Animal Research
Female BALB/c-nu/nu mice were used. On day 0, HT-29 cells or COLO205 cells suspended in ice-cold HBSS (-) were inoculated subcutaneously into the right flank of the mice at 5x10^6 cells/100 μl/site or 1x10^6 cells/100 μl/site, respectively. The acetic acid-solvated form of JTP-74057 was dissolved in 10% Cremophor EL-10% PEG400 and was administered orally once daily for 14 days from the day when the mean tumor volume reached 100 mm^3. The tumor length [L (mm)] and width [W (mm)] were measured using a micro gauge twice a week after the commencement of dosing, and the tumor volume was calculated using the following formula: tumor volume (mm^3) = L x W x W/2. All procedures relating to the use of animals in this study were reviewed and approved by the Institutional Animal Care and Use Committee of Japan Tobacco [1].
AliasGSK1120212, JTP-74057
Chemical Properties
Molecular Weight615.39
FormulaC26H23FIN5O4
Cas No.871700-17-3
Storage & Solubility Information
StoragePowder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.
Solubility Information
10% DMSO+40% PEG300+5% Tween 80+45% Saline: 2.1 mg/mL (3.41 mM), Suspension. Working solution is recommended to be prepared and used immediately.
DMSO: 7.86 mg/mL (12.77 mM)
Ethanol: < 1 mg/mL (insoluble or slightly soluble)
Solution Preparation Table
10% DMSO+40% PEG300+5% Tween 80+45% Saline/DMSO
1mg5mg10mg50mg
1 mM1.6250 mL8.1249 mL16.2499 mL81.2493 mL
DMSO
1mg5mg10mg50mg
5 mM0.3250 mL1.6250 mL3.2500 mL16.2499 mL
10 mM0.1625 mL0.8125 mL1.6250 mL8.1249 mL

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