英文名稱 | (E/Z)-Afatinib (Synonyms: (E/Z)-BIBW 2992; (S)-阿法替尼) |
---|---|
中文名稱 | (S)-N-(4-((3-氯-4-氟苯基)氨基(S)-N-(4-((3-四氫呋喃-3-基)氧基)喹唑啉-6-基)-4-(二甲基氨基)丁-2-烯酰胺 |
CAS號 | 439081-18-2 |
分子式 | C24H25ClFN5O3 |
分子量 | 485.94 |
外觀 | White to off-white powder |
儲存條件 | 4°C, protect from light |
英文名稱 | (E/Z)-Afatinib (Synonyms: (E/Z)-BIBW 2992; (S)-阿法替尼) |
---|---|
中文名稱 | (S)-N-(4-((3-氯-4-氟苯基)氨基(S)-N-(4-((3-四氫呋喃-3-基)氧基)喹唑啉-6-基)-4-(二甲基氨基)丁-2-烯酰胺 |
CAS號 | 439081-18-2 |
分子式 | C24H25ClFN5O3 |
分子量 | 485.94 |
外觀 | White to off-white powder |
儲存條件 | 4°C, protect from light |
(E/Z)-Afatinib ((E/Z)-BIBW 2992) is the mixture of (E)-Afatinib and (Z)-Afatinib. Afatinib (HY-10261) is an irreversible inhibitor of EGFR, by irreversibly binding to their ATP binding site to block activation of EGFR, HER2, HER4, and EGFRvIII. Afatinib used in co-administration with Temozolomide (HY-17364), potently targeting to EGFRvIII-cMet signaling in glioblastoma cells.
Preclinical evaluation of afatinib (BIBW2992) in esophageal squamous cell carcinoma (ESCC).
Am J Cancer Res. 2015 Nov 15;5(12):3588-99.
PMID: 25436978 PMCID: PMC4322967 DOI: 10.18632/oncotarget.2647
Antitumor activity of pan-HER inhibitors in HER2-positive gastric cancer.
PMID: 29465762 PMCID: PMC5891184 DOI: 10.1111/cas.13546
BIBW2992, an irreversible EGFR/HER2 inhibitor highly effective in preclinical lung cancer models.
PMID: 18408761 PMCID: PMC2748240 DOI: 10.1038/onc.2008.109