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Postion:Product Catalog >Pharmaceutical intermediates>Bulk Drug Intermediates>Trametinib (DMSO solvate)
Trametinib (DMSO solvate)
  • Trametinib (DMSO solvate)

Trametinib (DMSO solvate) NEW

Price $41 $57 $82
Package 10mg 50mg 100mg
Min. Order:
Supply Ability: 10g
Update Time: 2024-11-15

Product Details

Product Name: Trametinib (DMSO solvate) CAS No.: 1187431-43-1
Purity: 99.71% Supply Ability: 10g
Release date: 2024/11/15

Product Introduction

Bioactivity

名稱Trametinib (DMSO solvate)
描述Trametinib (DMSO solvate) (GSK-1120212 (DMSO solvate)) is a highly potent and selective MEK inhibitor that specifically inhibits MEK1/2 (IC50: 2 nM).
體外活性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.
體內(nèi)活性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.
存儲條件Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.
溶解度DMSO : 69 mg/mL (99.49 mM)
關(guān)鍵字Mitogen-activated protein kinase kinase | GSK 1120212 | JTP 74057 | arthritis | Apoptosis | JTP74057 | MAPKK | inhibit | DMSO solvate | Adjuvant-induced | Trametinib (DMSO solvate) | orally | Inhibitor | JTP-74057 | CIA | GSK1120212 | type | collageninduced | GSK-1120212 | AIA | MEK | Trametinib | MAP2K
相關(guān)產(chǎn)品Stavudine | 5-Fluorouracil | Acetylcysteine | Kaempferol | Myricetin | Sodium 4-phenylbutyrate | L-Ascorbic acid | Dextran sulfate sodium salt (MW 4500-5500) | Metronidazole | Sorafenib | Tributyrin | Lidocaine hydrochloride
相關(guān)庫神經(jīng)退行性疾病化合物庫 | 疼痛相關(guān)化合物庫 | EMA 上市藥物庫 | 激酶抑制劑庫 | 抗癌臨床化合物庫 | 藥物功能重定位化合物庫 | 抑制劑庫 | FDA 上市藥物庫 | 抗癌活性化合物庫 | 抗癌藥物庫

Company Profile Introduction

Target Molecule Corp. (TargetMol) is a global high-tech enterprise, headquartered in Boston, MA, specializing in chemical and biological research product and service to meet the research needs of global customers. TargetMol has evolved into one of the biggest global compound library and small molecule suppliers and a customer based on 40+ countries. TargetMol offers over 80 types of compound libraries and a wide range of high-quality research chemicals including inhibitors, activator, natural compounds, peptides, inhibitory antibodies, and novel life-science kits, for laboratory and scientific use. Besides, virtual screening service is also available for customers who would like to conduct the computer-aided drug discovery.

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