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抑制剂 > JAK STAT信令 > Afatinib(BIBW2992)
产品名称:
Afatinib(BIBW2992)
型号:
CS-01Y78442
生产地址
国产
产品价格
电议
产品简介
质量保证、价格优惠
产品详情

一、概述:

化学性质:                                                                                                             

规格

10mg 50mg 100mg 200mg

CAS

439081-18-2

别名

N/A

化学名

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

分子式

C24H25ClFN5O3

分子量

485.94

溶解度

24.3mg/mL in DMSO, 42.1 mg/mL in EtOH with ultrasonic

储存条件

Store at -20°C

General tips

For obtaining a higher solubility , please warm the tube at 37 and shake it in the ultrasonic bath for a while.

Shipping Condition

Evaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request

 

产品描述:                                                                                                            

Afatinib (BIBW2992), an irreversible inhibitor of the ErbB family of tyrosine kinases, downregulates ErbB signalling by binding to the kinase domains of epidermal growth factor receptor (EGFR)/ human epidermal growth factor receptor 2 (HER2) with IC50 of 0.5 nM and 14nM, respectively.

The ErbB receptor tyrosine kinase family consists of four cell surface receptors: ErbB1/ EGFR/HER1, ErbB2/HER2, ErbB3/HER3, and ErbB4/HER4. It has been shown that EGFR and HER2 play important roles in the development and progression of certain aggressive types of cancers and inflammation-associated diseases.

Afatinib was shown to suppress EGF-induced phosphorylation of EGFR and cell proliferation in a variety of EGFR-overexpressing and HER2-expressing cell lines such as A431, NIH-3T3-HER2, NCI-N87 and BT-474 [1].

The component has also been used extensively in various animal models to study the role of EGFR/HER2. Oral administration of afatinib inhibited cancer cell growth and survival and suppress the tumor regression in xenograft and transgenic lung cancer models [2]. In addition, afatinib is identified as EGFR blocker which was approved for the treatment of patients with EGFR-mutated nonsmall cell lung cancer [3].

特别提醒:                                                                                                              

1. 本产品仅供科研使用。请勿用于医药、临床诊断或治疗,食品及化妆品等用途。请勿存放于普通住宅区。

2. 为了您的安全和健康,请穿好实验服并佩戴一次性手套和口罩操作。

标签:Afatinib(BIBW2992) 

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