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Naquotinib mesylate

Catalog No. T12175   CAS 1448237-05-5
Synonyms: ASP8273 (mesylate)

Naquotinib mesylate (ASP8273 (mesylate)) is an orally available, mutant-selective and irreversible inhibitor of EGFR(iC50s of 8-33 nM and 230 nM for toward EGFR mutants and EGFR).

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Naquotinib mesylate Chemical Structure
Naquotinib mesylate, CAS 1448237-05-5
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Biological Description
Chemical Properties
Storage & Solubility Information
Description Naquotinib mesylate (ASP8273 (mesylate)) is an orally available, mutant-selective and irreversible inhibitor of EGFR(iC50s of 8-33 nM and 230 nM for toward EGFR mutants and EGFR).
Targets&IC50 EGFR:230 nM
In vitro In NCI-H1650 (del ex19), Naquotinib inhibits cell growth with an IC50 value of 70nM while other EGFR-TKIs are only partially effective.Naquotinib selectively inhibits phosphorylation of EGFR and its down-stream signal pathway, ERK and Akt from 10nM in HCC827 and NCI-H1975 while inhibitory effects are only detected at 1000nM in A431[2].
In vivo 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].
Synonyms ASP8273 (mesylate)
Molecular Weight 658.81
Formula C31H46N8O6S
CAS No. 1448237-05-5

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 12.5 mg/mL (18.97 mM), sonification/heating is recommended.

TargetMolReferences and Literature

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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Keywords

Naquotinib mesylate 1448237-05-5 Angiogenesis JAK/STAT signaling Tyrosine Kinase/Adaptors EGFR ErbB-1 ASP8273 (mesylate) Inhibitor ASP8273 ASP 8273 HER1 Epidermal growth factor receptor inhibit Naquotinib Mesylate ASP-8273 Naquotinib inhibitor

 

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