Naquotinib(ASP8273)

Catalog No.S8412

For research use only.

Naquotinib (ASP8273) is an orally available, irreversible, mutant-selective, epidermal growth factor receptor (EGFR) inhibitor, with potential antineoplastic activity.

Naquotinib(ASP8273) Chemical Structure

CAS No. 1448232-80-1

Selleck's Naquotinib(ASP8273) has been cited by 1 Publication

Purity & Quality Control

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Biological Activity

Description Naquotinib (ASP8273) is an orally available, irreversible, mutant-selective, epidermal growth factor receptor (EGFR) inhibitor, with potential antineoplastic activity.
Targets
mutant EGFR [1]
In vitro

ASP8273 is a small-molecule irreversible TKI inhibitor that inhibits the kinase activity of EGFR mutations including T790M, with limited activity against EGFR wild-type (WT) NSCLC. In the in vitro enzymatic and cell-based assays, ASP8273 is evaluated against EGFR mutants (L858R, exon 19 deletion, L858R/T790M, and del19/T790M) and WT EGFR. ASP8273 is found by mass spectrometry to covalently bind to a mutant EGFR (L858R/T790M) via cysteine residue 797 in the kinase domain of EGFR with long-lasting inhibition of EGFR phosphorylation for 24 h. In the NSCLC cell lines harboring the above EGFR mutations, ASP8273 has IC50 values of 8-33 nM toward EGFR mutants, more potently than that of WT EGFR (IC50 value of 230 nM). ASP8273 is further shown to suppress the signaling pathway through ERK and Akt. ASP8273 even shows activity in mutant EGFR cell line which is resistant to other EGFR TKIs including AZD9291 and CO-1686[1][2].

In vivo In mouse xenograft studies, ASP8273 induces tumor regression in NCI-H1975 (L858R/T790M), HCC827 (del ex19) and PC-9 (del ex19) xenograft models by repeated oral dosing in a dose-dependent manner. Dosing schedules do not affect the efficacy of ASP8273. In HCC827 and NCI-H1975 xenograft models, ASP8273 induces tumor regression at 10, 30 and 100mg/kg without affecting body weight. ASP8273 also produces tumor growth inhibition from 10mg/kg in the NSCLC patient derived tumor xenograft, LU1868 which express T790M/L858R. On the other hand, ASP8273 does not produce significant tumor growth inhibition at 10 and 30mg/kg in A431 xenograft model[1][2].

Protocol (from reference)

Solubility (25°C)

In vitro

Ethanol 100 mg/mL warmed
(177.71 mM)
DMSO 52 mg/mL warmed
(92.4 mM)
Water Insoluble

Chemical Information

Molecular Weight 562.71
Formula

C30H42N8O3

CAS No. 1448232-80-1
Storage 3 years -20°C powder
2 years -80°C in solvent
Smiles CCC1=C(N=C(C(=N1)C(=O)N)NC2=CC=C(C=C2)N3CCC(CC3)N4CCN(CC4)C)OC5CCN(C5)C(=O)C=C

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

mg/kg g μL

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO % % Tween 80 % ddH2O
%DMSO %

Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Molarity Calculator

Mass Concentration Volume Molecular Weight

Clinical Trial Information

NCT Number Recruitment Interventions Conditions Sponsor/Collaborators Start Date Phases
NCT03082300 Terminated Drug: naquotinib Non-small Cell Lung Cancer (NSCLC)|Epidermal Growth Factor Receptor (EGFR) Mutations Astellas Pharma Global Development Inc.|Astellas Pharma Inc March 24 2017 Phase 1
NCT02674555 Withdrawn Drug: radio-labeled naquotinib|Drug: naquotinib Epidermal Growth Factor Receptor (EGFR) Mutations|Solid Tumors Astellas Pharma Global Development Inc.|Astellas Pharma Inc November 15 2016 Phase 1
NCT02500927 Terminated Drug: ASP8273 Capsules|Drug: ASP8273 Capsules A EGFR-TKI-naïve Patients With NSCLC Harboring EGFR Activating Mutations Astellas Pharma Inc June 25 2015 Phase 2
NCT02113813 Completed Drug: naquotinib|Drug: midazolam Non-Small-Cell Lung Cancer (NSCLC)|Epidermal Growth Factor Receptor Mutations Astellas Pharma Global Development Inc.|Astellas Pharma Inc April 9 2014 Phase 1
NCT02192697 Terminated Drug: ASP8273 Non-small Cell Lung Cancer Astellas Pharma Inc January 23 2014 Phase 1|Phase 2

(data from https://clinicaltrials.gov, updated on 2022-01-17)

Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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