Mutant EGFR inhibitor - CAS 1421373-62-7
Catalog number: 1421373-62-7
Category: Inhibitor
Not Intended for Therapeutic Use. For research use only.
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Mutant EGFR inhibitor
1.EGFR-tyrosine kinase inhibitor treatment in a patient with advanced non-small cell lung cancer and concurrent exon 19 and 21 EGFR mutations: A case report and review of the literature.
Yang Y1, Zhang B2, Li R1, Liu B1, Wang L1. Oncol Lett. 2016 May;11(5):3546-3550. Epub 2016 Apr 5.
Epidermal growth factor receptor-tyrosine kinase inhibitors (EGFR-TKIs) are considered to be effective treatments for advanced non-small cell lung cancer (NSCLC) patients with sensitizing EGFR mutations, including exon 19 deletion and exon 21 L858R mutations. However, with the development of EGFR mutation detection assays, patients with complex EGFR mutations are emerging, and their response to EGFR-TKIs remains unclear. The present study reports a case of a 62-year-old, non-smoking female patient with advanced NSCLC, presenting with concurrent EGFR 19+21 sensitizing mutations, who had a poor response to the first-line EGFR-TKI erlotinib and succumbed 5 months subsequent to diagnosis. Furthermore, the present study performed a literature review, and 18 patients with complex EGFR 19+21 mutations that had received EGFR-TKIs were identified. The majority of these patients responded well to EGFR-TKIs. To the best of our knowledge, the present case is the first to report a patient with lung adenocarcinoma with complex EGFR 19+21 sensitizing mutations that had a poor clinical response to a first-line EGFR-TKI.
2.The Frequency of EGFR Mutation in Lung Adenocarcinoma and the Efficacy of Tyrosine Kinase Inhibitor Therapy in a Hungarian Cohort of Patients.
Sárosi V1, Balikó Z1, Smuk G2, László T2, Szabó M1, Ruzsics I1, Mezősi E3. Pathol Oncol Res. 2016 Apr 22. [Epub ahead of print]
In the last decades new therapeutic drugs have been developed for the treatment of non-small cell lung cancer (NSCLC) patients. Tyrosine kinase inhibitors (TKIs) significantly increase the progression free survival (PFS) of patients with NSCLC carrying epidermal growth factor receptor (EGFR) mutations. This type of lung cancer occurs mainly among non-smoking women and Asian origin. However, the new ESMO guideline recommends EGFR mutation analysis in every patient with NSCLC, because in patients with activating EGFR mutation, TKIs should be considered as first line therapy. In our recent work, we analyzed data of patients with EGFR-mutant adenocarcinoma from January 2009. The number of patients investigated was 446, among them 44 cases were positive for EGFR mutation. The ratio of positive cases was 9.86 % that is lower than the average mutation rate in Europe and much lower than that found in Asia. The exon 19 deletion was detected in 61.
3.Discovery of 5-(methylthio)pyrimidine derivatives as L858R/T790M mutant selective epidermal growth factor receptor (EGFR) inhibitors.
Xiao Q1, Qu R2, Gao D1, Yan Q1, Tong L2, Zhang W1, Ding J2, Xie H3, Li Y4. Bioorg Med Chem. 2016 Apr 19. pii: S0968-0896(16)30273-5. doi: 10.1016/j.bmc.2016.04.032. [Epub ahead of print]
To overcome the drug-resistance of first generation EGFR inhibitors and the nonselective toxicities of second generation inhibitors among NSCLC patients, a series of 5-(methylthio)pyrimidine derivatives were discovered as novel EGFR inhibitors, which harbored not only potent enzymatic and antiproliferative activities against EGFRL858R/T790M mutants, but good selectivity over wide-type form of the receptor. This goal was achieved by employing structure-based drug design and traditional optimization strategies, based on WZ4002 and CO1686. These derivatives inhibited the enzymatic activity of EGFRL858R/T790M mutants with IC50 values in subnanomolar ranges, while exhibiting hundreds of fold less potency on EGFRWT. These compounds also strongly inhibited the proliferation of H1975 non-small cell lung cancer cells bearing EGFRL858R/T790M, while being significantly less toxic to A431 human epithelial carcinoma cells with overexpressed EGFRWT. The EGFR kinase inhibitory and antiproliferative activities were further validated by Western blot analysis for activation of EGFR and the downstream signaling in cancer cells.
4.Pretreatment neutrophil-lymphocyte ratio is not a significant prognostic factor in epidermal growth factor receptor-mutant non-small cell lung cancer patients treated with tyrosine kinase inhibitors.
Sim SH1, Beom SH1, Ahn YO2, Keam B3, Kim TM3, Lee SH3, Kim DW3, Heo DS3. Thorac Cancer. 2016 Mar;7(2):161-6. doi: 10.1111/1759-7714.12304. Epub 2015 Aug 28.
BACKGROUND: The neutrophil-lymphocyte ratio (NLR) is a marker of poor prognosis in lung cancer patients. However, previous data have been based on an heterogeneous population of lung cancer patients and various treatments. In this study, we evaluate the prognostic value of NLR in an homogeneous population of epidermal growth factor receptor (EGFR)-mutant non-small cell lung cancer (NSCLC) patients.
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CAS 1421373-62-7 Mutant EGFR inhibitor

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