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Trametinib

Manufactured by Alsachim
Sourced in France

Trametinib is a chemical compound used as a laboratory reagent. It functions as a selective inhibitor of the mitogen-activated protein kinase (MEK) enzymes MEK1 and MEK2.

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3 protocols using trametinib

1

Dissolution and Dilution of BRAF Inhibitors

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Vemurafenib (PLX4032 or RG7204) was kindly donated by Roche for study purpose. Vemurafenib was dissolved in DMSO to a stock concentration of 1 mg/ml. The Vemurafenib stock was freshly diluted before each experiment to 60 μg/ml unless stated otherwise. Dabrafenib and trametinib were obtained from Alsachim (Illkirch-Graffenstaden, France). Both drugs were diluted freshly to 90 and 12 ng/ml, respectively.
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2

Trametinib administration protocol for in vivo study

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Trametinib (C3822, ALSACHIM) was dissolved in dimethyl sulfoxide (D4540; Sigma-Aldrich) to a concentration of 10 mM ( 6.15 mg/mL) and kept in aliquots at -80°C until use. On treatment day, an aliquot of working solution was thawed and added to sterile PBS for gavage. dimethyl sulfoxide was added to PBS for the vehicle treatment. Trametinib was administered daily over the course of 2 weeks (days 1-15 post-RT) at a concentration of 1 mg/kg body weight by oral gavage in 200 μL of total volume.
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3

Quantification of Oncology Drugs in Plasma

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The reference materials for alectinib, alectinib M4, AZ5104 (osimertinib active metabolite), Crizotinib-13C2D5, imatinib, imatinib-D8, and osimertinib were purchased from LGC Standards (Molsheim, France). Crizotinib, lorlatinib, methanol, and ammonium formate were obtained from Sigma-Aldrich (St-Quentin-Fallavier, France). Alectinib-D8, binimetinib, binimetinib-13CD4, cobimetinib, cobimetinib-13C6, dabrafenib, dabrafenib-D9, encorafenib, encorafenib-13C2D3, osimertinib-13CD3, trametinib, and trametinib-13C6 were provided from Alsachim (Illkirch Graffenstaden, France). Acetonitrile and formic acid came from VWR. Ultra-pure water (18 MΩ) was produced via ultrafiltration with a Q-Pod (Millipore Corp., Molsheim, France). All chemicals were of analytical grade. Blank human plasma samples were provided by a local blood bank (EFS, Versailles, France) and stored at −20 °C until analysis.
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