ChemicalBook > CAS DataBase List > FTI 277 HYDROCHLORIDE

FTI 277 HYDROCHLORIDE

Product Name
FTI 277 HYDROCHLORIDE
CAS No.
180977-34-8
Chemical Name
FTI 277 HYDROCHLORIDE
Synonyms
CS-1757;FTI 277 HCl;FTI 277 HCL;FTI 277;FTI 277 HYDROCHLORIDE;FTI-277 TRIFLUOROACETATE SALT;FTI 277 HYDROCHLORIDE USP/EP/BP;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;(S)-methyl 2-(5-(((R)-2-amino-3-mercaptopropyl)amino)-[1,1'-biphenyl]-2-ylcarboxamido)-4-(methylthio)butanoate hydrochloride;(S)-methyl 2-(5-(((R)-2-amino-3-mercaptopropyl)amino)-[1,1'-biphenyl]-2-ylcarboxamido)-4-(methylthio)butanoate hydrochloride
CBNumber
CB2503510
Molecular Formula
C22H30ClN3O3S2
Formula Weight
484.075
MOL File
180977-34-8.mol
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FTI 277 HYDROCHLORIDE Property

storage temp. 
Inert atmosphere,2-8°C
solubility 
H2O: soluble
form 
amorphous semi-solid
color 
White to off-white
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Safety

Hazard Codes 
Xi
Risk Statements 
36/37/38
Safety Statements 
26-36
WGK Germany 
3
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Hazard and Precautionary Statements (GHS)

Symbol(GHS)
Signal word
Warning
Hazard statements

H315Causes skin irritation

H319Causes serious eye irritation

H335May cause respiratory irritation

Precautionary statements

P261Avoid breathing dust/fume/gas/mist/vapours/spray.

P264Wash hands thoroughly after handling.

P264Wash skin thouroughly after handling.

P271Use only outdoors or in a well-ventilated area.

P280Wear protective gloves/protective clothing/eye protection/face protection.

P302+P352IF ON SKIN: wash with plenty of soap and water.

P304+P340IF INHALED: Remove victim to fresh air and Keep at rest in a position comfortable for breathing.

P305+P351+P338IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continuerinsing.

P312Call a POISON CENTER or doctor/physician if you feel unwell.

P362Take off contaminated clothing and wash before reuse.

P403+P233Store in a well-ventilated place. Keep container tightly closed.

P501Dispose of contents/container to..…

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N-Bromosuccinimide Price

ApexBio Technology
Product number
B5842
Product name
FTI277HCl
Packaging
2mg
Price
$126
Updated
2021/12/16
ChemScene
Product number
CS-3863
Product name
FTI-277(hydrochloride)
Purity
>99.0%
Packaging
5mg
Price
$132
Updated
2021/12/16
ApexBio Technology
Product number
B5842
Product name
FTI277HCl
Packaging
5mg
Price
$186
Updated
2021/12/16
ChemScene
Product number
CS-3863
Product name
FTI-277(hydrochloride)
Purity
>99.0%
Packaging
10mg
Price
$238
Updated
2021/12/16
ApexBio Technology
Product number
B5842
Product name
FTI277HCl
Packaging
10mg
Price
$312
Updated
2021/12/16
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FTI 277 HYDROCHLORIDE Chemical Properties,Usage,Production

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]

in vitro

FTI-277 inhibits Ras processing with an IC50 of 100 nM, but not the geranylgeranylated Rap1A processing in whole cells. It induces accumulation of cytoplasmic non-farnesylated H-Ras, accumulates inactive Ras/Raf complexes in the cytoplasm, and constitutive blocksive MAPK activation in H-RasF cells. It causes increased after irradiation and increases radiosensitivity in H-ras-transformed rat embryo cells. FTI-277 also inhibits cell growth and induces apoptosis in drug-resistant myeloma tumor cells. In SH- apoptosis SY5Y cells, It diminishes the toxic effects of methamphetamine on induction in cell degeneration, activation in c-Jun-N-terminal kinase cascades, and Ras activation.

in vivo

In mice coinfected with hepatitis B virus (HBV) and HDV, FTI-277 (50 mg/kg/d ip) effectively clears HDV viremia.

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.

FTI 277 HYDROCHLORIDE Preparation Products And Raw materials

Raw materials

Preparation Products

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180977-34-8, FTI 277 HYDROCHLORIDERelated Search:


  • CS-1757
  • 4-[2(R)-amino-3-mercaptopropyl]amino-2-phenylbenzoyl-(S)-methionine methyl ester hydrochloride
  • FTI 277 HYDROCHLORIDE
  • FTI-277 TRIFLUOROACETATE SALT
  • FTI 277 HCl
  • (S)-methyl 2-(5-(((R)-2-amino-3-mercaptopropyl)amino)-[1,1'-biphenyl]-2-ylcarboxamido)-4-(methylthio)butanoate FTI 277 HCl
  • FTI 277 HCL;FTI 277
  • FTI 277 HYDROCHLORIDE USP/EP/BP
  • (S)-methyl 2-(5-(((R)-2-amino-3-mercaptopropyl)amino)-[1,1'-biphenyl]-2-ylcarboxamido)-4-(methylthio)butanoate hydrochloride
  • (S)-methyl 2-(5-(((R)-2-amino-3-mercaptopropyl)amino)-[1,1'-biphenyl]-2-ylcarboxamido)-4-(methylthio)butanoate hydrochloride
  • 180977-34-8
  • C22H30ClN3O3S2
  • Inhibitors