180977-34-8

Basic information

• Product Name: FTI 277 HYDROCHLORIDE
• Synonyms: FTI 277 HYDROCHLORIDE;FTI-277 TRIFLUOROACETATE SALT;FTI 277 HCl;4-[2(R)-amino-3-mercaptopropyl]amino-2-phenylbenzoyl-(S)-methionine methyl ester hydrochloride;(S)-methyl 2-(5-(((R)-2-amino-3-mercaptopropyl)amino)-[1,1'-biphenyl]-2-ylcarboxamido)-4-(methylthio)butanoate FTI 277 HCl
• CAS NO: 180977-34-8
• Molecular Formula: C22H30ClN3O3S2
• Molecular Weight: 484.0749
• EINECS: 604-604-1
• Product Categories: Inhibitors
• Mol File: 180977-34-8.mol
• Article Data: 1

Chemical Properties

• Appearance: /amorphous semi-solid
• Storage Temp.: −20°C
• Solubility: H2O: soluble
• CAS DataBase Reference: FTI 277 HYDROCHLORIDE(CAS DataBase Reference)
• NIST Chemistry Reference: FTI 277 HYDROCHLORIDE(180977-34-8)
• EPA Substance Registry System: FTI 277 HYDROCHLORIDE(180977-34-8)

Safety Data

• Hazard Codes: Xi
• Statements: 36/37/38
• Safety Statements: 26-36
• WGK Germany: 3
• Hazardous Substances Data: 180977-34-8(Hazardous Substances Data)

Usage

Biological Activity

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 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.

Relevant articles and documents

Inhibitors of prenyl transferases

Compounds which inhibit prenyl transferases, particularly farnysyltransferase and geranylgeranyl transferase I, processes for preparing the compounds, pharmaceutical compositions containing the compounds, and methods of use.