GSK1120212 (DMSO solvate) NEW
| Price | $5 | $0.1 |
| Package | 1KG | 1000KG |
| Min. Order: | 1KG |
| Supply Ability: | g-kg-tons, free sample is available |
| Update Time: | 2024-03-26 |
Product Details
| Product Name: GSK1120212 (DMSO solvate) | CAS No.: 1187431-43-1 |
| Min. Order: 1KG | Purity: 98% |
| Supply Ability: g-kg-tons, free sample is available | Release date: 2024/03/26 |
| Lead time: In stock, ready for shipment | Packaging: bag/bottle/drum/IBC |
| Delivery: By express, by air, by sea | Origin: Manufacturer, advantage product |
| COA, MSDS: Available, contact us for details | Name: Tina |
1. Materials information
Names
| Name | trametinib dimethyl sulfoxide |
|---|---|
| Synonym | More Synonyms |
| Description | Trametinib DMSO solvate is a potent MEK inhibitor that specifically inhibits MEK1/2, with an IC50 value of about 2 nM. |
|---|---|
| Related Catalog |
Signaling Pathways >>
MAPK/ERK Pathway >>
MEK
Research Areas >>
Cancer
|
| Target |
MEK1:2 nM (IC50) MEK2:2 nM (IC50) |
| 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]. |
| Cell Assay | 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 Admin | 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 |
| Molecular Formula | C28H29FIN5O5S |
|---|---|
| Molecular Weight | 693.528 |
| Exact Mass | 693.091797 |
| PSA | 146.90000 |
| LogP | 5.52300 |
| Storage condition | 2-8℃ |
2. Packaging of materials
For powders: normal is 25kgs/Drum or bag, or larger/smaller package as request.
For liquids: normal 25kgs/drum, 180-300kgs/bucket, or IBC, determined by the nature of the product.
Or smaller package 1kg/bottle, 10kgs/bottle as request.
3. Shipping & Delivery
By Express
Provide door to door service
Suitable for goods under 50kg
Delivery: 3-7 days
Cost: low cost
By Air
Provide airport to airport service
Suitable for goods over 50kg
Delivery: 3-14 days
Cost: high cost
By Sea
Provide seaport to seaport service
Suitable for goods over 100kg
Delivery: 2-45 days
Cost: low cost
4. Contact information
For more details, pls contact us freely.
Email address: Tina@fdachem.com
Mob: 86 15225627621
WhatsApp/Skype/Wechat/LINE: 86 15225627621
Company Profile Introduction
Henan Fengda Chemical Co., Ltd. is located in the High-tech Development Zone of Henan Province. Specializing in the production and sales of various fine chemical products required for industrial production, including chemical raw materials, organic raw materials, petrochemicals, chemical reagents, solvents, catalysts, and additives, etc.
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China
- Since: 2023-02-10
- Address: Room 01, 2288 E05, Building 14, East Henan University, Science and Technology Park, 279 Xisanhuan Ro
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