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Trametinib (DMSO solvate)

🥰Excellent
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)

Trametinib (DMSO solvate)

🥰Excellent
Purity: 100%
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 SizePriceAvailabilityQuantity
10 mg38 â‚¬In Stock
25 mg51 â‚¬In Stock
50 mg54 â‚¬In Stock
100 mg77 â‚¬In Stock
200 mg111 â‚¬In Stock
1 mL x 10 mM (in DMSO)47 â‚¬In Stock
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Purity:100%
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Product Introduction

Bioactivity
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.
AliasTrametinib DMSO solvate, Trametinib dimethyl sulfoxide, JTP-74057 (DMSO solvate), GSK-1120212 (DMSO solvate)
Chemical Properties
Molecular Weight693.53
FormulaC28H29FIN5O5S
Cas No.1187431-43-1
SmilesCS(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 & Solubility Information
StoragePowder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.
Solubility Information
DMSO: 69 mg/mL (99.49 mM)
Solution Preparation Table
DMSO
1mg5mg10mg50mg
1 mM1.4419 mL7.2095 mL14.4190 mL72.0949 mL
5 mM0.2884 mL1.4419 mL2.8838 mL14.4190 mL
10 mM0.1442 mL0.7209 mL1.4419 mL7.2095 mL
20 mM0.0721 mL0.3605 mL0.7209 mL3.6047 mL
50 mM0.0288 mL0.1442 mL0.2884 mL1.4419 mL

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In Vivo Formulation Calculator (Clear solution)

Please enter your animal experiment information in the following box and click Calculate to obtain the mother liquor preparation method and in vivo formula preparation method:
TargetMol | Animal experimentsFor example, your dosage is 10 mg/kg Each animal weighs 20 g, and the dosage volume is 100 μL . TargetMol | Animal experiments A total of 10 animals were administered, and the formula you used is 5% TargetMol | reagent DMSO+30% PEG300+5% Tween 80+60% ddH2O. So your working solution concentration is 2 mg/mL。
Mother liquor preparation method: 2 mg of drug dissolved in 50 μL DMSOTargetMol | reagent (mother liquor concentration of 40 mg/mL), if you need to configure a concentration that exceeds the solubility of the product, please contact us first.
Preparation method for in vivo formula: Take 50 μL DMSOTargetMol | reagent main solution, add 300 μLPEG300TargetMol | reagent mix well and clarify, then add 50 more μL Tween 80, mix well and clarify, then add 600 more μLddH2OTargetMol | reagent mix well and clarify
For Reference Only. Please develop an appropriate dissolution method based on your laboratory animals and route of administration.
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2 Enter the in vivo formulation:
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