中英文说明丨艾美捷 LKT Labs 阿法替尼

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EGFR和EGFR2（HER2 / 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。

阿法替尼 基础信息：

编号：A2077

cas：850140-72-6;439081-18-2

纯度：≥98%

公式：C24H25ClFN5O3

配方重量：485.94

化学名称：N-[4-[（3-氯-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-氯-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.