产品名称

来那替尼(Neratinib)

一般描述

Neratinib(来那替尼) is a irreversible inhibitor of the HER-2 receptor tyrosine kinase with potential antineoplastic activity, and also a P-Glycoprotein Inhibitor.

别 称

(E)-N-[4-[3-chloro-4-(pyridin-2-ylmethoxy)anilino]-3-cyano-7-ethoxyquinolin-6-yl]-4-(dimethylamino)but-2-enamide; HKI-272; Nerlynx;

纯 度

≥98%(HPLC)

CAS NO.

698387-09-6

分子式

C³⁰H²⁹ClN⁶O³

分子量

557.051

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

~5mg/mL

乙醇

Insoluble

水

Insoluble

l  生物学信息

生物活性/药理作用

Neratinib is a tyrosine kinase inhibitor which exhibits antitumor action against Epidermal Growth Factor Receptor (EGFR), HER2, and Human Epidermal Growth Factor Receptor 4 (HER4) postive  carcinomas.

Neratinib is an orally available, 6,7-disubstituted-4-anilinoquinoline-3-carbonitrile irreversible inhibitor of the HER-2 receptor tyrosine kinase with potential antineoplastic activity.  Neratinib binds to the HER-2 receptor irreversibly, thereby reducing  autophosphorylation in cells, apparently by targeting a cysteine residue in the ATP-binding pocket of the receptor. Treatment of cells with this agent  results in inhibition of downstream signal transduction events and cell cycle regulatory pathways; arrest at the G1-S (Gap 1/DNA synthesis)-phase transition of the cell division cycle; and ultimately decreased cellular  proliferation. Neratinib also inhibits the epidermal growth factor receptor (EGFR) kinase and the proliferation of EGFR-dependent cells.

l  包装与存储

包 装

10mg; 50mg; 250mg

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