180977-34-8FTI 277 HCl

产品属性：

Cas No.180977-34-8

别名

化学名 (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

分子式 C22H30ClN3O3S2

分子量 484.07

溶解度 ≥ 100mg/mL in DMSO

储存条件 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.
Shipping Condition     Evaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
产品描述：
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.