Afatinib
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.
References PubMed ID：:http://www.ncbi.nlm.nih.gov/pubmed/18836992
| Cas No. |
850140-72-6 |
|---|---|
| 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 |
| Appearance |
Pale Yellow Powder |
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.
