產(chǎn)品目錄

規(guī)格	10mg 50mg 100mg 200mg
CAS	439081-18-2
別名	N/A
化學(xué)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
儲(chǔ)存條件	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

產(chǎn)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].

特別提醒：

1. 本產(chǎn)品僅供科研使用。請(qǐng)勿用于醫(yī)藥、臨床診斷或治療，食品及化妝品等用途。請(qǐng)勿存放于普通住宅區(qū)。

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原創(chuàng)作者：上海莼試生物技術(shù)有限公司

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