您好,欢迎来到试剂信息网! [登录] [免费注册]
试剂信息网
位置:首页 > 产品库 > FTI-277 hydrochloride
立即咨询
咨询类型:
     
*姓名:
*电话:
*单位:
Email:
*留言内容:
请详细说明您的需求。
*验证码:
 
FTI-277 hydrochloride
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
FTI-277 hydrochloride图片
CAS NO:180977-34-8
包装与价格:
包装价格(元)
1 mg电议
2 mg电议
5 mg电议
10 mg电议
25 mg电议
50 mg电议
100 mg电议
1 mL*10 mM(in DMSO)电议

产品名称
FTI 277 HCl
产品介绍
FTI-277 hydrochloride 是一种法尼基转移酶FTase抑制剂,高效 Ras CAAX 肽模拟物,可抑制H-Ras和K-Ras信号转导,还可抑制hepatitis delta virus 感染。

产品描述

FTI 277 hydrochloride is an effective and specific farnesyltransferase (FTase) inhibitor (IC50: 500 pM); this selectivity is about 100-fold than the closely related GGTase I.

体外活性

在感染乙型肝炎病毒和丁型肝炎病毒的小鼠体内,FTI-277(50 mg/kg/day,i.p.)可有效清除丁型肝炎病毒血症.

体内活性

在耐药骨髓瘤细胞中,FTI-277对细胞生长有抑制作用,还诱导细胞凋亡。在SH-SY5细胞中,FTI-277对细胞退化、活化、c-Jun-N端激酶级联和Ras激活过程中甲基苯丙胺诱导的毒性有减弱作用。FTI-277抑制Ras加工(IC50:100 nM),但对全细胞中四异戊二烯化Rap1A加工无影响。FTI-277导致辐射后细胞凋亡增加,并使H-ras转化的大鼠胚胎细胞的辐射敏感性增加。

激酶实验

FTase and GGTase I Activity Assay: FTase and GGTase I activities from 60,000×g supernatants of human Burkitt lymphoma (Daudi) cells are assayed. Inhibition studies are performed by determining the ability of Ras CAAX peptidomimetics to inhibit the transfer of [3H]farnesyl and [3H]geranylgeranyl from [3H]farnesylpyrophosphate and [3H]geranylgeranylpyrophosphate to H-Ras-CVLS and H-Ras-CVLL, respectively.

细胞实验

Cells are seeded at 8000–14 000 cells/well in 96-well plates. To establish a dose–response to FTI-277, cells are incubated for 96 h in two-fold serial dilutions ranging from 3.75 times 10-7 M to 1 times 10-5 M. Following continuous drug exposure, 50 μL MTT dye is added. The insoluble formazan complex is solubilized with DMSO and absorbance measured at 540 nm. IC50s and 95% confidence intervals are calculated by regression analysis of the linear portion of the dose–response curve. (Only for Reference)

Cas No.

180977-34-8

分子式

C22H30ClN3O3S2

分子量

484.07

别名

FTI 277 HCl

储存和溶解度

H2O:14 mg/mL (28.9 mM)
Ethanol:12 mg/mL (24.8 mM)
DMSO:89 mg/mL (183.9 mM)
Powder: -20°C for 3 years
In solvent: -80°C for 2 years