| Identification | Back Directory | [Name]
Naquotinib (mesylate) | [CAS]
1448237-05-5 | [Synonyms]
ASP8273 (mesylate)
Naquotinib (mesylate)
Naquotinib mesylate (ASP8273 mesylate) | [Molecular Formula]
C31H46N8O6S | [MDL Number]
MFCD30496702 | [MOL File]
1448237-05-5.mol | [Molecular Weight]
658.812 |
| Hazard Information | Back Directory | [Uses]
Naquotinib mesylate (ASP8273 mesylate) is an orally available, mutant-selective and irreversible EGFR inhibitor; with IC50s of 8-33 nM toward EGFR mutants and 230 nM for EGFR. | [in vivo]
Oral Naquotinib treatment dose dependently induces tumor regression in NCI-H1975 (L858R/T790M), HCC827 (del ex19) and PC-9 (del ex19) xenograft models. Dosing schedules does not affect the efficacy of Naquotinib. In an NCI-H1975 xenograft model, complete regression of tumor is achieved after 14-days of Naquotinib treatment. Complete regression is maintained in 50% of mice more than 85 days after cessation of Naquotinib treatment[2]. | [IC 50]
EGFRL858R/T790M; EGFRL858R; EGFRExon 19 deletion; EGFRExon 19 deletion/T790M; EGFR: 230 nM (IC50) | [References]
[1] Sakagami H, et al. ASP8273, a novel mutant-selective irreversible EGFR inhibitor, inhibits growth of non-small cell lung cancer (NSCLC) cells with EGFR activating and T790M resistance mutations. [abstract]. In: Proceedings of the 105th Annual Meeting of the American Association for Cancer Research; 2014 Apr 5-9; San Diego, CA. Philadelphia (PA): AACR; Cancer Res 2014;74(19 Suppl):Abstract nr 1728. doi:10.1158/1538-7445.AM2014-1728
[2] Konagai S, et al. ASP8273 selectively inhibits mutant EGFR signal pathway and induces tumor shrinkage in EGFR mutated tumor models. [abstract]. In: Proceedings of the 106th Annual Meeting of the American Association for Cancer Research; 2015 Apr 18-22; Philadelphia, PA. Philadelphia (PA): AACR; Cancer Res 2015;75(15 Suppl):Abstract nr 2586. doi:10.1158/1538-7445.AM2015-2586 |
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