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FTI 277 HClFTase inhibitor

FTI 277 HCl

Catalog No. B5842
Size Price Stock Qty
5mg $103.00 In stock
25mg $334.00 In stock
100mg $698.00 In stock

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Sample solution is provided at 25 µL, 10mM.

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Chemical structure

FTI 277 HCl

FTI 277 HCl Dilution Calculator

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Chemical Properties

Cas No. 180977-34-8 SDF Download SDF
Chemical 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
Canonical SMILES COC([C@](/N=C(O)/C1=C(C2=CC=CC=C2)C=C(NC[C@](N)([H])CS)C=C1)([H])CCSC)=O.Cl
Formula C22H30ClN3O3S2 M.Wt 484.07
Solubility Soluble in DMSO Storage Store at -20°C
General tips For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.
Shipping Condition Evaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request

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]

References:
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 blocks
oncogenic Ras signaling by inducing cytoplasmic accumulation of inactive Ras-Raf complexes.  J Biol Chem. 1995 Nov 10;270(45):26802-6. PubMed PMID: 7592920.