Name: FTI 277 HCl
Price: 280.00 USD

- Overview
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    Background
    
    FTI-277 is a highly potent and selective FTase inhibitor. At concentration as low as 10 nM, FTI-277 inhibits H-Ras processing and the processing is blocked by more than 95% at 3 μM. [1]
    Ras proteins are plasma membrane-associated GTPases. It acts as relay switches transducing biological information from extracellular signals to the nucleus. Farnesyltransferase (FTase) is an enzyme that catalyzed the Ras farnesylation, a lipid posttranslational modification that is required for Ras-induced malignant transformation. [1]
    FTI-277, the methyl ester derivative of FTI-276, is extremely potent (ICGraphic = 100 nM) at inhibiting H-Ras, but not the geranylgeranylated Rap1A processing in whole cells. FTI-277 is a farnesylation-specific inhibitor which inhibits the processing of both oncogenic and normal Ras. [1]
    In mice that hydrodynamically transfected to produce Hepatitis delta virus (HDV) viremia, FTI-277 treatment is effective in inhibiting viremia. [2]
    
    1. Bordier BB, Ohkanda J, Liu P et al. In vivo antiviral efficacy of prenylation inhibitors against hepatitis delta virus. J Clin Invest. 2003 Aug;112(3):407-14.
    2. Lerner EC, Qian Y, Blaskovich MA et al. Ras CAAX peptidomimetic FTI-277 selectively blocksoncogenic Ras signaling by inducing cytoplasmic accumulation of inactive Ras-Raf complexes. J Biol Chem. 1995 Nov 10;270(45):26802-6. PubMed PMID: 7592920.
- Properties
  - Alternative Name
    
    (Z)-5-(((R)-2-amino-3-mercaptopropyl)amino)-N-((S)-1-methoxy-4-(methylthio)-1-oxobutan-2-yl)-[1,1'-biphenyl]-2-carbimidic acid hydrochloride
    
    CAS Number
    
    180977-34-8
    
    Molecular Formula
    
    C22H30ClN3O3S2
    
    Molecular Weight
    
    484.07
    
    Purity
    
    98.00%
    
    Solubility
    
    ≥0.67 mg/mL in H2O with ultrasonic; ≥100 mg/mL in DMSO; ≥4.6 mg/mL in EtOH
    
    Storage
    
    Store at -20°C
    
    * For Research Use Only

FTI 277 HCl

FTI 277 HCl

Background

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