产品名称

阿法替尼双马来酸盐(Afatinib diMaleate)

一般描述

Afatinib Dimaleate is the dimaleate salt form of afatinib, an orally bioavailable anilino-quinazoline derivative and inhibitor of the receptor tyrosine kinase (RTK) epidermal growth factor receptor (ErbB; EGFR) family, with antineoplastic activity.

化学名称

(Z)-but-2-enedioic acid; (E)-N-[4-(3-chloro-4-fluoroanilino)-7-[(3S)-oxolan-3-yl]oxyquinazolin-6-yl]-4-(dimethylamino)but-2-enamide. BIBW2992 DiMaleate.

纯 度

≥99% (HPLC)

CAS NO.

850140-73-7

分子式

C²⁴H²⁵ClFN⁵O³·2(C⁴H⁴O⁴)

分子量

717.18

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

溶解度(25℃)

DMSO

≥50mg/mL

乙醇

Very slightly soluble

水

Very slightly soluble

l  生物学信息

生物活性/药理作用

Afatinib Dimaleate is the dimaleate salt form of afatinib, 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; 100mg; 500mg

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.    https://ncit.nci.nih.gov

2.    https://pubchem.ncbi.nlm.nih.gov