产品名称

阿法替尼(Afatinib)

一般描述

Afatinib is an orally bioavailable inhibitor of the receptor tyrosine kinase (RTK) epidermal growth factor receptor (ErbB; EGFR) family, with antineoplastic activity.

别 称

(E)-N-[4-(3-chloro-4-fluoroanilino)-7-[(3S)-oxolan-3-yl]oxyquinazolin-6-yl]-4-(dimethylamino)but-2-enamide;  BIBW2992;Tovok;

纯 度

≥98%(HPLC)

CAS NO.

439081-18-2

分子式

C²⁴H²⁵ClFN⁵O³

分子量

485.944

适用范围

生物试剂，适用于细胞培养等

l  理化信息

外 观

白色或类白色至黄色固体

溶解性(25℃)

DMSO

≥50mg/mL

乙醇

≥15mg/mL

水

Insoluble

l  生物学信息

生物活性/药理作用

Afatinib is an orally bioavailable anilino-quinazoline derivative and inhibitor of the receptor tyrosine kinase  (RTK) epidermal growth factor receptor (ErbB; EGFR) family, with antineoplastic  activity. Upon administration, afatinib selectively and irreversibly binds to and inhibits the epidermal growth factor receptors 1 (ErbB1; EGFR), 2 (ErbB2;  HER2), and 4 (ErbB4; HER4), and certain EGFR mutants, including those caused  by EGFR exon 19 deletion mutations or exon 21 (L858R) mutations. This may result in the inhibition of tumor growth and angiogenesis in tumor cells overexpressing these RTKs. Additionally, afatinib inhibits the EGFR T790M gatekeeper mutation which is resistant to treatment with first-generation  EGFR inhibitors. EGFR, HER2 and HER4 are RTKs that belong to the EGFR  superfamily; they play major roles in both tumor cell proliferation and tumor vascularization and are overexpressed in many cancer cell types.

l  包装与存储

包 装

25mg; 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