Afatinib - CAS 850140-72-6
Catalog number: 850140-72-6
Category: Inhibitor
Not Intended for Therapeutic Use. For research use only.
Molecular Formula:
C24H25ClFN5O3
Molecular Weight:
485.94
COA:
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Targets:
EGFR
Description:
Afatinib irreversibly inhibits EGFR/HER2 including EGFR, EGFR(L858R), EGFR(L858R/T790M) and HER2. It is 100-fold more active against Gefitinib-resistant L858R-T790M EGFR mutant.
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Purity:
>98%
Synonyms:
BIBW-2992
MSDS:
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1.Afatinib versus methotrexate in older patients with second-line recurrent and/or metastatic head and neck squamous cell carcinoma: subgroup analysis of the LUX-Head & Neck 1 trial.
Clement PM1, Gauler T2, Machiels JH3, Haddad RI4, Fayette J5, Licitra LF6, Tahara M7, Cohen EE8, Cupissol D9, Grau JJ10, Guigay J11, Caponigro F12, de Castro G Jr13, de Souza Viana L14, Keilholz U15, Del Campo JM16, Cong XJ17, Ehrnrooth E18, Vermorken JB1 Ann Oncol. 2016 Apr 15. pii: mdw151. [Epub ahead of print]
BACKGROUND: In the phase III LUX-Head & Neck 1 (LHN1) trial, afatinib significantly improved progression-free survival (PFS) versus methotrexate in recurrent and/or metastatic (R/M) head and neck squamous cell carcinoma (HNSCC) patients progressing on/after platinum-based therapy. This report evaluates afatinib efficacy and safety in pre-specified subgroups of patients aged ≥65 and <65 years.
2.In vitro and in vivo efficacy of afatinib as a single agent or in combination with gemcitabine for the treatment of nasopharyngeal carcinoma.
Xue C1, Tian Y2, Zhang J3, Zhao Y1, Zhan J2, Fang W1, Zhang L1. Drug Des Devel Ther. 2016 Mar 31;10:1299-306. doi: 10.2147/DDDT.S94432. eCollection 2016.
PURPOSE: Epidermal growth factor receptor (EGFR) is usually overexpressed in nasopharyngeal carcinoma (NPC). We tested the antitumor effects of irreversible ErbB family inhibitor afatinib on human NPC using in vitro and in vivo models.
3.Afatinib in first-line setting for NSCLC harbouring common EGFR mutations: new light after the preliminary results of LUX-Lung 7?
Passaro A1, Pochesci A1, Spitaleri G1, Catania C1, Noberasco C1, Del Signore E1, de Marinis F1. J Thorac Dis. 2016 Mar;8(3):E217-20. doi: 10.21037/jtd.2016.02.21.
The development of epidermal growth factor receptor (EGFR) tyrosine kinase inhibitors (TKIs) changed dramatically the history of non-small cell lung cancer (NSCLC) harboring EGFR sensitive mutations. Several randomized prospective trials confirmed the superiority of these target agents about survival and response rate when comparing with platinum-based chemotherapy. Knowledge about EGFR mutations increased gradually during the development of target agents and different clinical trials. EGFR mutations cannot be considered all equal, but different entities should be considered in our clinical practice: exon 19 deletions, exon 21 mutation (L858R) and uncommon mutation (exon 20, exon 18 and double mutation). Nowadays, we dispose of three different EGFR TKIs (afatinib, erlotinib and gefitinib) approved for the treatment for first-line treatment of patients di NSCLC carrying EGFR, that was compared only by indirect analysis, producing data not always clear and convincing.
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CAS 850140-72-6 Afatinib

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