Molecular Weight(MW): 562.71
Naquotinib(ASP8273) is an orally available, irreversible, mutant-selective, epidermal growth factor receptor (EGFR) inhibitor, with potential antineoplastic activity.
Purity & Quality Control
Choose Selective EGFR Inhibitors
|Description||Naquotinib(ASP8273) is an orally available, irreversible, mutant-selective, epidermal growth factor receptor (EGFR) inhibitor, with potential antineoplastic activity.|
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.
|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.|
|In vitro||Ethanol||100 mg/mL warmed (177.71 mM)|
|DMSO||52 mg/mL warmed (92.4 mM)|
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Clinical Trial Information
|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|
|NCT03042013||Withdrawn||Subjects With NSCLC With an EGFR Activating Mutation||Astellas Pharma Global Development Inc.|Astellas Pharma Inc||February 28 2017||Phase 2|
|NCT02674555||Withdrawn||Epidermal Growth Factor Receptor (EGFR) Mutations|Solid Tumors||Astellas Pharma Global Development Inc.|Astellas Pharma Inc||November 15 2016||Phase 1|
|NCT02588261||Terminated||Non-small Cell Lung Cancer (NSCLC)||Astellas Pharma Global Development Inc.|Astellas Pharma Inc||February 11 2016||Phase 3|
|NCT02500927||Terminated||EGFR-TKI-naïve Patients With NSCLC Harboring EGFR Activating Mutations||Astellas Pharma Inc||June 25 2015||Phase 2|
|NCT02113813||Active not recruiting||Non-Small-Cell Lung Cancer (NSCLC)|Epidermal Growth Factor Receptor Mutations||Astellas Pharma Global Development Inc.|Astellas Pharma Inc||April 23 2014||Phase 1|
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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