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Naquotinib(ASP8273)

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

Naquotinib(ASP8273) Chemical Structure

Naquotinib(ASP8273) Chemical Structure

CAS No. 1448232-80-1

Purity & Quality Control

Batch: S841201 Ethanol]100 mg/mL]false]DMSO]52 mg/mL]false]Water]Insoluble]false Purity: 99.43%
99.43

Naquotinib(ASP8273) Related Products

Signaling Pathway

EGFR Signaling Pathways

EGFR Signaling Pathway

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
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 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].
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT03082300 Terminated
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
Epidermal Growth Factor Receptor (EGFR) Mutations|Solid Tumors
Astellas Pharma Global Development Inc.|Astellas Pharma Inc
 November 15 2016 Phase 1
NCT02500927 Terminated
EGFR-TKI-naïve Patients With NSCLC Harboring EGFR Activating Mutations
Astellas Pharma Inc
 June 25 2015 Phase 2
NCT02113813 Completed
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
Non-small Cell Lung Cancer
Astellas Pharma Inc
 January 23 2014 Phase 1|Phase 2

Chemical Information & Solubility

Molecular Weight 562.71 Formula

C30H42N8O3
CAS No. 1448232-80-1 SDF Download Naquotinib(ASP8273) SDF
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
Storage (From the date of receipt)

In vitro
Batch:

Ethanol : 100 mg/mL

DMSO : 52 mg/mL ( (92.4 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : Insoluble


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In vivo
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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.

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