产品名称

替吡法尼(Tipifarnib)

一般描述

Tipifarnib(替吡法尼),  a nonpeptidomimetic quinolinone, is a specific farnesyltransferase (FTase)  inhibitor with potential antineoplastic activity.

别 称

6-[(R)-amino-(4-chlorophenyl)-(3-methylimidazol-4-yl)methyl]-4-(3-chlorophenyl)-1-methylquinolin-2-one;  Zarnestra;  R115777; R-115777

纯 度

≥98%(HPLC)

CAS NO.

192185-72-1

分子式

C²⁷H²²Cl²N⁴O

分子量

489.4

适用范围

生物试剂，适用于细胞培养等

l  理化信息

外 观

白色或类白色固体

溶解性(25℃)

DMSO

≥10mg/mL

乙醇

Insoluble

水

Insoluble

l  生物学信息

生物活性/药理作用

R115777, a nonpeptidomimetic farnesyl transferase inhibitor, suppresses the growth of human pancreatic adenocarcinoma cell lines. This growth inhibition is associated with modulation in the phosphorylation levels of signal transducers and activators  of tranion 3 (STAT3) and extracellular signal-regulated kinases (ERK).

Tipifarnib is a nonpeptidomimetic quinolinone with potential antineoplastic activity. Tipifarnib binds to and inhibits the enzyme farnesyl protein transferase, an enzyme involved in protein processing (farnesylation) for signal transduction. By inhibiting the  farnesylation of proteins, this agent prevents the activation of Ras  oncogenes, inhibits cell growth, induces apoptosis, and inhibits angiogenesis.

l  包装与存储

包 装

2mg; 5mg; 25mg

存储温度

-20℃

l  注意事项及免责声明

本产品仅用于实验研究，不得作为药物使用，不得用于家用或其它用途。

l  参考文献

1.    http://www.drugbank.ca

2.    https://ncit.nci.nih.gov

3.   https://www.ncbi.nlm.nih.gov