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Naquotinib

Catalog No. TQ0092   CAS 1448232-80-1
Synonyms: ASP8273

Naquotinib (ASP8273) (ASP8273) is an orally available, mutant-selective and irreversible EGFR inhibitor; (IC50s: 8-33 nM and 230 nM toward EGFR mutants and EGFR.

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Naquotinib Chemical Structure
Naquotinib, CAS 1448232-80-1
Pack Size Availability Price/USD Quantity
1 mg In stock $ 43.00
2 mg In stock $ 61.00
5 mg In stock $ 98.00
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1 mL * 10 mM (in DMSO) In stock $ 135.00
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Purity: 97.49%
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Biological Description
Chemical Properties
Storage & Solubility Information
Description Naquotinib (ASP8273) (ASP8273) is an orally available, mutant-selective and irreversible EGFR inhibitor; (IC50s: 8-33 nM and 230 nM toward EGFR mutants and EGFR.
Targets&IC50 EGFR:230 nM, EGFR mutants:8-33 nM
In vitro In assays using endogenously EGFR-dependent cells, Naquotinib inhibits the growth of PC-9(del ex19), HCC827(del ex19), NCI-H1975(del ex19/T790M) and PC-9ER(del ex19/T790M) with IC50s of 8-33 nM [1]. Naquotinib selectively inhibits phosphorylation of EGFR and its downstream signal pathway, ERK, and Akt from 10nM in HCC827 and NCI-H1975 while inhibitory effects are only detected at 1000nM in A431.In NCI-H1650 (del ex19), Naquotinib inhibits cell growth with an IC50 value of 70nM while other EGFR-TKIs are only partially effective [2].
In vivo In NCI-H1975 (L858R/T790M), HCC827 (del ex19) and PC-9 (del ex19) xenograft models, oral Naquotinib treatment dose-dependently induces tumor regression. Dosing schedules do 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].
Synonyms ASP8273
Molecular Weight 562.71
Formula C30H42N8O3
CAS No. 1448232-80-1

Storage

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

Solubility Information

H2O: Insoluble

H2O: Insoluble

Ethanol: 80 mg/mL (142.16 mM)

DMSO: 40 mg/mL (71.08 mM)

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

Related compound libraries

This product is contained In the following compound libraries:
Anti-Cancer Active Compound Library Highly Selective Inhibitor Library Anti-Cancer Drug Library Anti-Cancer Clinical Compound Library Tyrosine Kinase Inhibitor Library Anti-Breast Cancer Compound Library Anti-Prostate Cancer Compound Library Orally Active Compound Library ReFRAME Related Library Anti-Lung Cancer Compound Library

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EGFR-IN-9 ARRY-380 (analog ) Boehmenan Theliatinib Marinobufogenin Cyasterone (Rac)-JBJ-04-125-02 Mavelertinib

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Keywords

Naquotinib 1448232-80-1 Angiogenesis JAK/STAT signaling Tyrosine Kinase/Adaptors EGFR Epidermal growth factor receptor HER1 ErbB-1 ASP-8273 inhibit ASP8273 ASP 8273 Inhibitor inhibitor

 

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