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Naquotinib Naquotinib is an irreversible, third-generation, mutant-selective, epidermal growth factor receptor (EGFR) inhibitor, with potential antineoplastic activity with IC50 of 8-33 nM toward EGFR mutants. Synonyms: ASP 8273; ASP8273; ASP-8273; (R)-5-((1-acryloylpyrrolidin-3-yl)oxy)-6-ethyl-3-((4-(4-(4-methylpiperazin-1-yl)piperidin-1-yl)phenyl)amino)pyrazine-2-carboxamide. Grades: ≥98%. CAS No. 1448232-80-1. Molecular formula: C30H42N8O3. Mole weight: 562.719. BOC Sciences 8
Naquotinib mesylate Naquotinib is irreversible, third-generation, epidermal growth factor receptor (EGFR) inhibitor with IC50 value of 70 nM for NCI-H1650 cell growth. It can covalently bind to and inhibit the activity of mutant forms of EGFR, including the T790M EGFR mutant. So Naquotinib can prevent EGFR-mediated signaling. This may induce cell death and inhibit tumor growth in EGFR-overexpressing tumor cells. In Dec 2015, Phase-III clinical trials in Non-small cell lung cancer (First-line therapy, Late-stage disease) in Hungary was on-going. In Aug 2016, Phase-I clinical trials in Solid tumours in USA was on-going. Uses: Solid tumours;non-small cell lung cancer. Synonyms: ASP8273 mesilate; ASP 8273 mesilate; ASP-8273 mesilate; 6-Ethyl-3-((4-(4-(4-methylpiperazin-1-yl)piperidin-1-yl)phenyl)amino)-5-(((3R)-1-(1-oxoprop-2-en-1-yl)pyrrolidin-3-yl)oxy)pyrazine-2-carboxamide monomethanesulfonate;448232-80-1 (free base). Grades: 98%. CAS No. 1448237-05-5. Molecular formula: C31H46N8O6S. Mole weight: 658.82. BOC Sciences 10

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