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Trametinib DMSO solvate

Allosteric MEK1/MEK2 kinase inhibitor CAS# 1187431-43-1

Trametinib DMSO solvate

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Product Name & Size Price Stock
Trametinib DMSO solvate:10mg $49.00 In stock
Trametinib DMSO solvate:20mg $83.00 In stock
Trametinib DMSO solvate:50mg $196.00 In stock
Trametinib DMSO solvate:100mg $343.00 In stock
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Quality Control of Trametinib DMSO solvate

Quality Control & MSDS

Number of papers citing our products

Chemical structure

Trametinib DMSO solvate

3D structure

Chemical Properties of Trametinib DMSO solvate

Cas No. 1187431-43-1 SDF Download SDF
PubChem ID 50992434 Appearance Powder
Formula C28H29FIN5O5S M.Wt 693.53
Type of Compound N/A Storage Desiccate at -20°C
Synonyms GSK-1120212 DMSO solvate; Trametinib; JTP-74057; GSK1120212
Solubility DMSO : 69 mg/mL (99.49 mM; Need ultrasonic)
H2O : < 0.1 mg/mL (insoluble)
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
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
Standard InChIKey OQUFJVRYDFIQBW-UHFFFAOYSA-N
Standard InChI InChI=1S/C26H23FIN5O4.C2H6OS/c1-13-22-21(23(31(3)24(13)35)30-20-10-7-15(28)11-19(20)27)25(36)33(17-8-9-17)26(37)32(22)18-6-4-5-16(12-18)29-14(2)34;1-4(2)3/h4-7,10-12,17,30H,8-9H2,1-3H3,(H,29,34);1-2H3
General tips For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.
We recommend that you prepare and use the solution on the same day. However, if the test schedule requires, the stock solutions can be prepared in advance, and the stock solution must be sealed and stored below -20℃. In general, the stock solution can be kept for several months.
Before use, we recommend that you leave the vial at room temperature for at least an hour before opening it.
About Packaging 1. The packaging of the product may be reversed during transportation, cause the high purity compounds to adhere to the neck or cap of the vial.Take the vail out of its packaging and shake gently until the compounds fall to the bottom of the vial.
2. For liquid products, please centrifuge at 500xg to gather the liquid to the bottom of the vial.
3. Try to avoid loss or contamination during the experiment.
Shipping Condition Packaging according to customer requirements(5mg, 10mg, 20mg and more). Ship via FedEx, DHL, UPS, EMS or other couriers with RT, or blue ice upon request.

Biological Activity of Trametinib DMSO solvate

DescriptionTrametinib DMSO solvate is a potent MEK inhibitor that specifically inhibits MEK1/2, with an IC50 value of about 2 nM.In Vitro:In BRAF mutant SK-MEL-28 cells and KRAS mutant HCT116 cells, Trametinib (GSK1120212) DMSO solvate causes dose-dependent inhibition of ERK1/2 phosphorylation as well as dose-dependent growth inhibition. In both SK-MEL-28 and HCT116 cells, Trametinib DMSO solvate inhibits 50% p-ERK1/2 at nearly equivalent concentrations (0.8 and 1.8 nM, respectively). However, as the slopes of the curves reflect, in SK-MEL-28 cells, Trametinib DMSO solvate inhibits 90% p-ERK1/2 at a lower concentration (3.4 nM) than in HCT116 (33.3 nM). Furthermore, in both cell lines, 50% growth inhibition is only achieved at concentrations Trametinib DMSO solvate that produces near complete ERK1/2 inhibition (85 and 90%, respectively)[2].In Vivo:Trametinib (GSK1120212) DMSO solvate is evaluated in vivo in an A549 (KRAS mutant cell line) xenograft model, orally dosing daily for 21 days (qd×21). In this study, near complete tumor growth inhibition is observed at 5.0 and 2.5 mg/kg [92 and 87% tumor growth inhibition (TGI), respectively] and to a lesser degree at 0.5 and 0.1 mg/kg (62 and 58% TGI). Although 5 mg/kg is the maximally tolerated dose (MTD) in this study, 3 mg/kg is the typically observed MTD. Dose-dependent antitumor activity with Trametinib DMSO solvate treatment has been similarly reported for several other KRAS and BRAF mutant tumor models[2].

References:
[1]. Yamaguchi T, et al. Suppressive effect of an orally active MEK1/2 inhibitor in two different animal models for rheumatoid arthritis: a comparison with leflunomide. Inflamm Res, 2012, 61(5), 445-454. [2]. Abe H, et al. Discovery of a Highly Potent and Selective MEK Inhibitor: GSK1120212 (JTP-74057 DMSO Solvate). ACS Med Chem Lett. 2011 Feb 28;2(4):320-4.

Protocol

Cell Assay [2]
SK-MEL-28, and HCT116 cell lines are plated in triplicate 96 well microtitre plates at 5000 cells per well in culture media. Trametinib dissolved in DMSO or negative control (0.1% DMSO) are added the following day and one plate is harvested with 50 μL of CellTiter-Glo for a time 0 (T=0) measurement. Remaining duplicate cell plates are typically incubated for 72 h. Cells are then lysed with 50 μL CellTiter-Glo, and chemiluminescent signal is read on the Wallac EnVision 2100 plate reader. For measurement of cellular ERK1/2 phosphorylation, cells are seeded and treated with Trametinib, and lysed after 72 h in Tris lysis buffer supplemented with phosphatase and protease inhibitors. All samples are analyzed with a phospho-ERK1/2 ELISA. Plates are read on MSD.SI6000 and curves are analyzed using the XLfit curve-fitting tool. For comparison of the growth assay curve and pERK1/2 assay curve, data are background subtracted and normalized to the vehicle treatment control[2].

Animal Administration [2]
Mice[2] A549 (human non-small cell lung carcinoma) model is established from cells grown in tissue culture and harvested aseptically using a trypsin digest. Female athymic mice (strain nu/nu) are injected subcutaneously with between 5×106 and 107 cells in 50% martigel. Tumors are allowed to establish for one to four weeks before use. Trametinib is administered orally at the indicated doses in 0.2 mL/20 g by weight. Tumors are measured twice weekly using Vernier calipers. Antitumor activity is defined as tumor growth inhibition representing the % volume differential in tumor growth between the treated and control tumors at the time vehicle tumors exceeded a volume of 1000 mm3.

References:
[1]. Yamaguchi T, et al. Suppressive effect of an orally active MEK1/2 inhibitor in two different animal models for rheumatoid arthritis: a comparison with leflunomide. Inflamm Res, 2012, 61(5), 445-454. [2]. Abe H, et al. Discovery of a Highly Potent and Selective MEK Inhibitor: GSK1120212 (JTP-74057 DMSO Solvate). ACS Med Chem Lett. 2011 Feb 28;2(4):320-4.

Trametinib DMSO solvate Dilution Calculator

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Trametinib DMSO solvate Molarity Calculator

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Preparing Stock Solutions of Trametinib DMSO solvate

1 mg 5 mg 10 mg 20 mg 25 mg
1 mM 1.4419 mL 7.2095 mL 14.419 mL 28.838 mL 36.0475 mL
5 mM 0.2884 mL 1.4419 mL 2.8838 mL 5.7676 mL 7.2095 mL
10 mM 0.1442 mL 0.7209 mL 1.4419 mL 2.8838 mL 3.6047 mL
50 mM 0.0288 mL 0.1442 mL 0.2884 mL 0.5768 mL 0.7209 mL
100 mM 0.0144 mL 0.0721 mL 0.1442 mL 0.2884 mL 0.3605 mL
* Note: If you are in the process of experiment, it's necessary to make the dilution ratios of the samples. The dilution data above is only for reference. Normally, it's can get a better solubility within lower of Concentrations.

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Background on Trametinib DMSO solvate

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

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Description

Trametinib (DMSO solvate) (GSK-1120212 (DMSO solvate);JTP-74057 (DMSO solvate)) is an orally active MEK inhibitor that inhibits MEK1 and MEK2 with IC50s of about 2 nM. Trametinib (DMSO solvate) activates autophagy and induces apoptosis.

Keywords:

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