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Trametinib DMSO solvateAllosteric MEK1/MEK2 kinase inhibitor

Trametinib DMSO solvate

Catalog No. A3887
Size Price Stock Qty
10mM (in 1mL DMSO) $55.00 In stock
10mg $50.00 In stock
50mg $80.00 In stock
100mg $119.00 In stock

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Sample solution is provided at 25 µL, 10mM.

Quality Control

Chemical structure

Trametinib DMSO solvate

Protocol

Kinase experiment [1]:

Raf-MEK-ERK cascade kinase assay

Non-phosphorylated 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 ERERK2 in 10 μM ATP and 12.5 mM MgCl2 containing MOPS buffer in the presence of various concentrations of Trametinib. The phosphorylation of MBP was detected by the anti-phospho-MBP antibody.

Cell experiment [1]:

Cell lines

HT-29 and COLO205 cells

Preparation method

This compound is soluble in DMSO. General tips for obtaining a higher concentration: Please warm the tube at 37℃ for 10 minutes and/or shake it in the ultrasonic bath for a while. Stock solution can be stored below -20℃ for several months.

Reaction Conditions

0, 1, 10 and 100 nM; 0 ~ 4 days

Applications

Trametinib induced apoptosis both in HT-29 and COLO205 cells, but that COLO205 cells were more sensitive to Trametinib than HT-29 cells in terms of apoptosis induction.

Animal experiment [1]:

Animal models

Female BALB/c-nu/nu mice inoculated subcutaneously with HT-29 or COLO205 cells

Dosage form

0.3 or 1 mg/kg; p.o.; q.d., for 14 days

Applications

Oral administration of Trametinib (0.3 or 1 mg/kg, q.d., for 14 days) was effective in inhibiting the HT-29 xenograft growth, and 1 mg/kg of Trametinib almost completely blocked the tumor increase. In the COLO205 xenograft model, tumor regression was observed even at a dose of 0.3 mg/kg. At a dosage of 1 mg/kg, a complete regression was obtained in 4 out of 6 mice in which the tumor degenerated to the point that tumor volume was not measurable.

Other notes

Please test the solubility of all compounds indoor, and the actual solubility may slightly differ with the theoretical value. This is caused by an experimental system error and it is normal.

References:

[1]. Yamaguchi T, Kakefuda R, Tajima N, Sowa Y, Sakai T. 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.

Trametinib DMSO solvate Dilution Calculator

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Chemical Properties

Cas No. 1187431-43-1 SDF Download SDF
Synonyms GSK-1120212 DMSO solvate;Trametinib;JTP-74057;GSK-1120212;GSK1120212;GSK 1120212;JTP 74057;JTP74057
Chemical Name N-[3-[3-cyclopropyl-5-(2-fluoro-4-iodoanilino)-6,8-dimethyl-2,4,7-trioxopyrido[4,3-d]pyrimidin-1-yl]phenyl]acetamide;methylsulfinylmethane
Canonical SMILES CC1=C2C(=C(N(C1=O)C)NC3=C(C=C(C=C3)I)F)C(=O)N(C(=O)N2C4=CC(=CC=C4)NC(=O)C)C5CC5.CS(=O)C
Formula C28H29FIN5O5S M.Wt 693.53
Solubility >11.6mg/mL in DMSO Storage Store at -20°C
General tips No
Shipping Condition No

Background

Trametinib (also known as GSK1120212 or JTP 74057), originally identified as a p15 inductive compound, is a novel and potent allosteric inhibitor of MEK kinase, which exhibits ATP non-competitive inhibition against MEK1 and MEK2 kinase. It has demonstrated broad antitumor activities in a variety of tumor xgenograft models, including HT-29 and COLO205 colorectal tumor cell lines. Trametinib induces expression of p15 and p27, reduces cyclin D1 levels, and causes dephosphorylation of RB protein and G1-phase arrest with a reduction of TS expression in HT-29 cells. It also effectively inhibits p-ERK 1/2 resulting in cell growth inhibition in tumor cell lines harboring B-RAF mutant.
Reference
1.Akintunde Akinleye, Muhammad Furqan, Nikhil Mukhi, Pavan Ravella and Delong Liu. MEK and the inhibitors: from bench to bedside. Journal of Hematology & Oncology 2013, 6:27
2.Motoki Watanabe, Yoshihiro Sowa, Mayumi Yogosawa and Toshiyuki Sakai. Novel MEK inhibitor trametinib and other retinoblastoma gene (RB)-reactivating agents enhance efficacy of 5-fluorouracil on human colon cancer cells. Cancer Sci 2013; 104(6): 687-693