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Trametinib (DMSO solvate)
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Catalog No. T5857Cas No. 1187431-43-1
Alias Trametinib DMSO solvate, Trametinib dimethyl sulfoxide, JTP-74057 (DMSO solvate), GSK-1120212 (DMSO solvate)
Trametinib (DMSO solvate) (GSK-1120212 (DMSO solvate)) is a highly potent and selective MEK inhibitor that specifically inhibits MEK1/2 (IC50: 2 nM).
Trametinib (DMSO solvate)
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Purity: 99.92%
Catalog No. T5857Alias Trametinib DMSO solvate, Trametinib dimethyl sulfoxide, JTP-74057 (DMSO solvate), GSK-1120212 (DMSO solvate)Cas No. 1187431-43-1
Trametinib (DMSO solvate) (GSK-1120212 (DMSO solvate)) is a highly potent and selective MEK inhibitor that specifically inhibits MEK1/2 (IC50: 2 nM).
| Pack Size | Price | USA Warehouse | Global Warehouse | Quantity |
|---|---|---|---|---|
| 10 mg | $41 | In Stock | In Stock | |
| 25 mg | $54 | In Stock | In Stock | |
| 50 mg | $57 | In Stock | In Stock | |
| 100 mg | $82 | In Stock | In Stock | |
| 200 mg | $117 | - | In Stock |
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In Stock Estimated shipping dateUSA Warehouse[1-2 days] Global Warehouse[5-7 days]
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Purity:99.92%
Appearance:Solid
Color:White
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Product Introduction
Bioactivity
Chemical Properties
Storage & Solubility Information
| Description | Trametinib (DMSO solvate) (GSK-1120212 (DMSO solvate)) is a highly potent and selective MEK inhibitor that specifically inhibits MEK1/2 (IC50: 2 nM). |
| Targets&IC50 | MEK1/2:2 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. |
| Synonyms | Trametinib DMSO solvate, Trametinib dimethyl sulfoxide, JTP-74057 (DMSO solvate), GSK-1120212 (DMSO solvate) |
| Molecular Weight | 693.53 |
| Formula | C28H29FIN5O5S |
| Cas No. | 1187431-43-1 |
| Smiles | CS(C)=O.CC(=O)Nc1cccc(c1)-n1c2c(C)c(=O)n(C)c(Nc3ccc(I)cc3F)c2c(=O)n(C2CC2)c1=O |
| Relative Density. | no data available |
| Storage | keep away from direct sunlight,keep away from moisture,store at low temperature | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature. | ||||||||||
| Solubility Information | DMSO: 1.3 mg/mL (1.87 mM), Sonication is recommended.  | ||||||||||
| In Vivo Formulation | 10% DMSO+40% PEG300+5% Tween 80+45% Saline: 1 mg/mL (1.44 mM), Sonication is recommended. Please add the solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately. The formulation provided above is for reference purposes only. In vivo formulations may vary and should be modified based on specific experimental conditions. | ||||||||||
Solution Preparation Table | |||||||||||
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Calculator
In Vivo Formulation Calculator (Clear solution)
Please enter your animal experiment information in the following box and click Calculate to obtain the stock solution preparation method and in vivo formula preparation method:
For example, if the intended dosage is 10 mg/kg for animals weighing 20 g , with a dosing volume of 100 μL per animal, and a total of 10 animals are to be administered, using a formulation of 
10% DMSO+ 40% PEG300+ 5% Tween 80+ 45% Saline/PBS/ddH2O , the resulting working solution concentration would be 2 mg/mL.Stock Solution Preparation:
Dissolve 2 mg of the compound in 100 μL DMSO to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.
Preparation of the In Vivo Formulation:
1) Add 100 μL of the DMSO stock solution to 400 μL PEG300 and mix thoroughly until the solution becomes clear.
2) Add 50 μL Tween 80 and mix well until fully clarified.
3) Add 450 μL Saline,PBS or ddH2O and mix thoroughly until a homogeneous solution is obtained.
This example is provided solely to demonstrate the use of the In Vivo Formulation Calculator and does not constitute a recommended formulation for any specific compound. Please select an appropriate dissolution and formulation strategy based on your experimental model and route of administration.
Dose Conversion
You can also refer to dose conversion for different animals. More Dose Conversion
Tech Support
Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc
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