| Name | Trametinib (DMSO solvate) |
| Description | Trametinib (DMSO solvate) (GSK-1120212 (DMSO solvate)) is a highly potent and selective MEK inhibitor that specifically inhibits MEK1/2 (IC50: 2 nM). |
| In vitro | Trametinib DMSO solvate displays remarkable potency in cellular assays for ERK1/2 phosphorylation and growth inhibition and excellent in vivo activity.?Inhibition of the MEK?ERK pathway offers a very promising therapeutic strategy for cancers with activating mutant Ras and Raf, and GSK1120212 (DMSO solvate) has been advanced into phase III trials for advanced or metastatic BRAF mutant melanoma as well as phase I and II studies in subjects with solid tumors or leukemia. |
| In vivo | Trametinib DMSO solvate was then evaluated in vivo in an A549 (KRAS mutant cell line) xenograft model, orally dosing daily for 21 days (qd × 21).Near complete tumor growth inhibition was 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).?[Notably, although 5 mg/kg was the maximally tolerated dose (MTD) , 3 mg/kg is the typically observed MTD.] Dose-dependent antitumor activity with GSK1120212 (DMSO solvate) treatment has been similarly reported for several other KRAS and BRAF mutant tumor models. |
| Storage | Shipping with blue ice/Shipping at ambient temperature. |
| Solubility Information | DMSO : 1.3 mg/mL (1.87 mM), Sonication is recommended.
10% DMSO+40% PEG300+5% Tween 80+45% Saline : 1 mg/mL (1.44 mM), Sonication is recommended.
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| Keywords | type | Trametinib (DMSO solvate) | Trametinib | orally | Mitogen-activated protein kinase kinase | MEK1/2 | MEK | MAPKK | MAP2K | JTP-74057 | JTP74057 | JTP 74057 | Inhibitor | inhibit | GSK-1120212 | GSK1120212 | GSK 1120212 | DMSO solvate | collageninduced | CIA | arthritis | Apoptosis | AIA | Adjuvant-induced |
| Inhibitors Related | Stavudine | Aceglutamide | Urea | Tamoxifen | Cysteamine hydrochloride | Metronidazole | Citric Acid Triammonium | Formamide | Dimethyl phthalate | Alginic acid | Sodium Molybdate | Sildenafil citrate |
| Related Compound Libraries | Failed Clinical Trials Compound Library | Bioactive Compound Library | Anti-Neurodegenerative Disease Compound Library | EMA Approved Drug Library | Anti-Cancer Clinical Compound Library | Drug Repurposing Compound Library | Anti-Cancer Approved Drug Library | FDA-Approved Kinase Inhibitor Library | Immunology/Inflammation Compound Library | Bioactive Compounds Library Max | Anti-Cancer Drug Library | Anti-Cancer Active Compound Library |
United States
