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武汉艾美捷科技有限公司

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中英文说明丨艾美捷 LKT Labs 阿法替尼

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发布日期:2023/5/24 17:35:17

更新日期:2023/5/24 17:35:17

详细内容

 Afatanib is an anticancer chemotherapeutic compound that has been approved to treat advanced lung cancers such as non-small cell lung cancer (NSCLC) and is in clinical trials as a potential treatment for other advanced solid tumors such as breast cancer and colorectal cancer. Afatanib exerts its anticancer activity through inhibition of EGFR and EGFR2 (HER2/ErbB2). In vivo, afatanib downregulates expression of HER2, increasing apoptosis and decreasing tumor size.

 

Product Info

Cas No. 850140-72-6; 439081-18-2

Purity 98%

Formula C24H25ClFN5O3

Formula Wt. 485.94

Chemical Name

N-[4-[(3-Chloro-4-fluorophenyl)amino]-7-[[(3S)-tetrahydro-3-furanyl]oxy]-6-quinazolinyl]-4(dimethylamino)-2-butenamide

IUPAC Name

(2E)-N-{4-[(3-Chloro-4-fluorophenyl)amino]-7-[(3S)-tetrahydro-3-furanyloxy]-6-quinazolinyl}-4-(dimethylamino)-2-butenamide

Synonym BIBW 2992

Melting Point 130-142°C

Appearance Pale Yellow Powder

 

艾美捷 LKT Labs 阿法替尼 是一种抗癌化疗化合物,已被批准用于治疗晚期肺癌,如非小细胞肺癌(NSCLC),并正在临床试验中,作为其他晚期实体瘤(如乳腺癌和结直肠癌)的潜在治疗方法。阿法替尼通过抑制EGFREGFR2HER2 / ErbB2)发挥其抗癌活性。在体内,阿法坦尼下调HER2的表达,增加细胞凋亡并减小肿瘤大小。

 

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阿法替尼 基础信息:

编号:A2077

cas850140-72-6;439081-18-2

纯度:≥98%

公式:C24H25ClFN5O3

配方重量:485.94

化学名称:N-[4-[3--4-氟苯基)氨基]-7-[[3S-四氢-3-呋喃氧基]-6-喹唑啉基]-4(二甲氨基)-2-丁烯酰胺

IUPAC名称:(2E-N-4-[3--4-氟苯基)氨基]-7-[3S-四氢-3-呋喃氧基]-6-喹唑啉基}-4-(二甲氨基)-2-丁烯酰胺

同义词:青苗 2992

熔点:130-142°C

外观:淡黄色粉末

 

阿法替尼文献参考:

Yap TA, Popat S. The role of afatinib in the management of non-small cell lung carcinoma. Expert Opin Drug Metab Toxicol. 2013 Nov;9(11):1529-39. PMID: 23985030.

 

Janjigian YY, Viola-Villegas N, Holland JP, et al. Monitoring afatinib treatment in HER2-positive gastric cancer with 18F-FDG and 89Zr-trastuzumab PET. J Nucl Med. 2013 Jun;54(6):936-43. PMID: 23578997.

 

Solca F, Dahl G, Zoephel A, et al. Target binding properties and cellular activity of afatinib (BIBW 2992), an irreversible ErbB family blocker. J Pharmacol Exp Ther. 2012 Nov;343(2):342-50. PMID: 22888144.

 

Hirsh V. Afatinib (BIBW 2992) development in non-small-cell lung cancer. Future Oncol. 2011 Jul;7(7):817-25. PMID: 21732753.

 

来源:https://www.amyjet.com/products/LKT-A2077-100mg.shtml

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