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
FTI 277 HYDROCHLORIDE Property
- storage temp.
- Inert atmosphere,2-8°C
- solubility
- H2O: soluble
- form
- amorphous semi-solid
- color
- White to off-white
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..…
N-Bromosuccinimide Price
- Product number
- B5842
- Product name
- FTI277HCl
- Packaging
- 2mg
- Price
- $126
- Updated
- 2021/12/16
- Product number
- CS-3863
- Product name
- FTI-277(hydrochloride)
- Purity
- >99.0%
- Packaging
- 5mg
- Price
- $132
- Updated
- 2021/12/16
- Product number
- B5842
- Product name
- FTI277HCl
- Packaging
- 5mg
- Price
- $186
- Updated
- 2021/12/16
- Product number
- CS-3863
- Product name
- FTI-277(hydrochloride)
- Purity
- >99.0%
- Packaging
- 10mg
- Price
- $238
- Updated
- 2021/12/16
- Product number
- B5842
- Product name
- FTI277HCl
- Packaging
- 10mg
- Price
- $312
- Updated
- 2021/12/16
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.
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