Name: Trametinib DMSO solvate
Price: 188.00 USD

- Overview
  - Please contact us at for specific academic pricing.
    
    Background
    
    Trametinib (also known as GSK1120212 or JTP 74057), originally identified as a p15 inductive compound, is a novel and potent allosteric inhibitor of MEK kinase, which exhibits ATP non-competitive inhibition against MEK1 and MEK2 kinase. It has demonstrated broad antitumor activities in a variety of tumor xgenograft models, including HT-29 and COLO205 colorectal tumor cell lines. Trametinib induces expression of p15 and p27, reduces cyclin D1 levels, and causes dephosphorylation of RB protein and G1-phase arrest with a reduction of TS expression in HT-29 cells. It also effectively inhibits p-ERK 1/2 resulting in cell growth inhibition in tumor cell lines harboring B-RAF mutant.
- Properties
  - Alternative Name
    
    GSK-1120212 DMSO solvate;Trametinib;JTP-74057;GSK-1120212;GSK1120212;GSK 1120212;JTP 74057;JTP74057; N-[3-[3-cyclopropyl-5-(2-fluoro-4-iodoanilino)-6,8-dimethyl-2,4,7-trioxopyrido[4,3-d]pyrimidin-1-yl]phenyl]acetamide;methylsulfinylmethane
    
    CAS Number
    
    1187431-43-1
    
    Molecular Formula
    
    C28H29FIN5O5S
    
    Molecular Weight
    
    693.53
    
    Appearance
    
    A solid
    
    Purity
    
    99.78%
    
    Solubility
    
    insoluble in EtOH; insoluble in H2O; ≥11.2 mg/mL in DMSO with gentle warming and ultrasonic
    
    Storage
    
    Store at -20°C
    
    * For Research Use Only
- Reference
  - 1. Lee PC, Fang YF, et al. "Targeting PKCδ as a Therapeutic Strategy against Heterogeneous Mechanisms of EGFR Inhibitor Resistance in EGFR-Mutant Lung Cancer." Cancer Cell. 2018 Dec 10;34(6):954-969.e4. PMID:30537515

Trametinib DMSO solvate

Trametinib DMSO solvate

Background

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