中英文說明丨艾美捷 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.
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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
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艾美捷?LKT Labs?阿法替尼?是一種抗癌化療化合物，已被批準用于治療晚期肺癌，如非小細胞肺癌（NSCLC），并正在臨床試驗中，作為其他晚期實體瘤（如乳腺癌和結直腸癌）的潛在治療方法。阿法替尼通過抑制EGFR和EGFR2（HER2 / ErbB2）發(fā)揮其抗癌活性。在體內(nèi)，阿法坦尼下調(diào)HER2的表達，增加細胞凋亡并減小腫瘤大小。
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阿法替尼?基礎信息：
編號：A2077
cas：850140-72-6;439081-18-2
純度：≥98%
公式：C24H25ClFN5O3
配方重量：485.94
化學名稱：N-[4-[（3-氯-4-氟苯基）氨基]-7-[[（3S）-四氫-3-呋喃氧基]-6-喹唑啉基]-4（二甲氨基）-2-丁烯酰胺
IUPAC名稱：（2E）-N-4-[（3-氯-4-氟苯基）氨基]-7-[（3S）-四氫-3-呋喃氧基]-6-喹唑啉基}-4-（二甲氨基）-2-丁烯酰胺
同義詞：青苗?2992
熔點：130-142°C
外觀：淡黃色粉末
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阿法替尼文獻參考：
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.
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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.
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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.
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Hirsh V. Afatinib (BIBW 2992) development in non-small-cell lung cancer. Future Oncol. 2011 Jul;7(7):817-25. PMID: 21732753.
