产品名称

吉非替尼(Gefitinib)

一般描述

Gefitinib(吉非替尼) is a selective tyrosine kinase receptor inhibitor used in the therapy of non-small cell lung cancer.

别 称

N-(3-chloro-4-fluorophenyl)-7-methoxy-6-(3-morpholin-4-ylpropoxy)quinazolin-4-amine;  AKOS 91371;Iressa; ZD1839; Irressat;ZD-1839

纯 度

≥99%(HPLC)

CAS NO.

184475-35-2

分子式

C²²H²⁴ClFN⁴O³

分子量

446.907

适用范围

生物试剂，适用于细胞培养等

l  理化信息

外 观

白色至类白色固体

溶解性(25℃)

DMSO

≥50mg/mL

乙醇

~4mg/mL

水

Insoluble

l  生物学信息

生物活性/药理作用

Gefitinib inhibits the intracellular phosphorylation of numerous tyrosine kinases associated with transmembrane cell surface receptors, including the tyrosine kinases associated with the  epidermal growth factor receptor (EGFR-TK). EGFR is expressed on the cell surface of many normal cells and cancer cells.

Gefitinib is an anilinoquinazoline with antineoplastic activity. Gefitinib inhibits the catalytic activity of  numerous tyrosine kinases including the epidermal growth factor receptor  (EGFR), which may result in inhibition of tyrosine kinase-dependent tumor  growth. Specifically, this agent competes with the binding of ATP to the tyrosine kinase domain of EGFR, thereby inhibiting receptor autophosphorylation and resulting in inhibition of signal transduction. Gefitinib may also induce cell cycle arrest and inhibit angiogenesis.

l  包装与存储

包 装

250mg; 1g

存储温度

0-5℃

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