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Trametinib

Catalog No. T2125   CAS 871700-17-3
Synonyms: GSK1120212, JTP-74057

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 products from TargetMol are for Research Use Only. Not for Human or Veterinary or Therapeutic Use.
Trametinib Chemical Structure
Trametinib, CAS 871700-17-3
Pack Size Availability Price/USD Quantity
5 mg In stock $ 31.00
10 mg In stock $ 50.00
50 mg In stock $ 64.00
100 mg In stock $ 100.00
200 mg In stock $ 141.00
1 mL * 10 mM (in DMSO) In stock $ 50.00
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Purity: 99.88%
Purity: 99.72%
Purity: 99.71%
Purity: 99.39%
Purity: 98%
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Biological Description
Chemical Properties
Storage & Solubility Information
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].
Synonyms GSK1120212, JTP-74057
Molecular Weight 615.39
Formula C26H23FIN5O4
CAS No. 871700-17-3

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 21 mg/mL (34.1 mM)

Ethanol: < 1 mg/mL (insoluble or slightly soluble)

TargetMolReferences and Literature

1. Wabitsch S, et al. Anti-PD-1 in Combination With Trametinib Suppresses Tumor Growth and Improves Survival of Intrahepatic Cholangiocarcinoma in Mice. Cell Mol Gastroenterol Hepatol. 2021;12(3):1166-1178. 2. Jing J, et al. Comprehensive predictive biomarker analysis for MEK inhibitor GSK112021Mol Cancer Ther. 2012 Mar;11(3):720-9. 3. Gao M, et al. Trametinib Inhibits the Growth and Aerobic Glycolysis of Glioma Cells by Targeting the PKM2/c-Myc Axis. Front Pharmacol. 2021 Oct 21;12:760055. 4. Yamaguchi T, et al. Antitumor activities of JTP-74057 (GSK1120212), a novel MEK1/2 inhibitor, on colorectal cancer cell lines in vitro and in vivo. Int J Oncol. 2011 Jul;39(1):23-31. 5. Kerstjens M, et al. Trametinib inhibits RAS-mutant MLL-rearranged acute lymphoblastic leukemia at specific niche sites and reduces ERK phosphorylation in vivo. Haematologica. 2018 Apr;103(4):e147-e150. 6. Wang X, Wu F, Wang H, et al. PDCD6 cooperates with C-Raf to facilitate colorectal cancer progression via Raf/MEK/ERK activation[J]. Journal of Experimental & Clinical Cancer Research. 2020, 39(1): 1-15.

TargetMolCitations

1. Jiang Z, Cheng L, Wu Z, et al. Transforming primary human hepatocytes into hepatocellular carcinoma with genetically defined factors. EMBO reports. 2022: e54275 2. Wang X, Wu F, Wang H, et al. PDCD6 cooperates with C-Raf to facilitate colorectal cancer progression via Raf/MEK/ERK activation. Journal of Experimental & Clinical Cancer Research. 2020, 39(1): 1-15 3. Sun C Y, Li Y Z, Cao D, et al. Rapamycin and trametinib: a rational combination for treatment of NSCLC. International Journal of Biological Sciences. 2021, 17(12): 3211-3223. 4. Lü Z, Li X, Li K, et al. Nitazoxanide and related thiazolides induce cell death in cancer cells by targeting the 20S proteasome with novel binding modes. Biochemical Pharmacology. 2022: 114913. 5. Klein C, Roussel G, Brun S, et al. 5-HIAA induces neprilysin to ameliorate pathophysiology and symptoms in a mouse model for Alzheimer’s disease. Acta Neuropathologica Communications. 2018 Dec 11;6(1):136 6. KieΔling M K, Nicolay J P, Schlör T, et al. NRAS mutations in cutaneous T cell lymphoma (CTCL) sensitize tumors towards treatment with the multikinase inhibitor Sorafenib. Oncotarget. 2017 Jul 11;8(28):45687-45697. 7. Meng Y, Lv T, Zhang J, et al.Temporospatial inhibition of Erk signaling is required for lymphatic valve formation.Signal Transduction and Targeted Therapy.2023, 8(1): 342.

Related compound libraries

This product is contained In the following compound libraries:
Anti-Cancer Approved Drug Library Tyrosine Kinase Inhibitor Library Highly Selective Inhibitor Library Anti-Neurodegenerative Disease Compound Library Anti-Cancer Clinical Compound Library Anti-Cancer Drug Library Anti-Cancer Active Compound Library Preclinical Compound Library FDA-Approved & Pharmacopeia Drug Library Fluorochemical Library

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Keywords

Trametinib 871700-17-3 Apoptosis Autophagy MAPK MEK inhibit MAP2K Inhibitor GSK1120212 orally type MAPKK collageninduced arthritis AIA GSK 1120212 JTP74057 Mitogen-activated protein kinase kinase GSK-1120212 JTP-74057 Adjuvant-induced JTP 74057 CIA inhibitor

 

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