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Naquotinib

CAS No. 1448232-80-1

Naquotinib( ASP8273 )

Catalog No. M11913 CAS No. 1448232-80-1

Naquotinib (ASP-8273) is a potent, irreversible, mutant-selective inhibitor of EGFR.

Purity : >98% (HPLC)

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Biological Information

  • Product Name
    Naquotinib
  • Note
    Research use only, not for human use.
  • Brief Description
    Naquotinib (ASP-8273) is a potent, irreversible, mutant-selective inhibitor of EGFR.
  • Description
    Naquotinib (ASP-8273) is a potent, irreversible, mutant-selective inhibitor of EGFR (IC50=8-33 nM for (L858R, exon 19 deletion, L858R/T790M, and del19/T790M)); more potently than that of WT EGFR (IC50= 230 nM); shows activity in mutant EGFR cell line which is resistant to other EGFR TKIs including AZD9291 and CO-1686.Lung Cancer Phase 1 Discontinued.
  • 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. 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.In NCI-H1650 (del ex19), Naquotinib inhibits cell growth with an IC50 value of 70nM while other EGFR-TKIs are only partially effective.
  • In Vivo
    Oral Naquotinib treatment dose dependently induces tumor regression in NCI-H1975 (L858R/T790M), HCC827 (del ex19) and PC-9 (del ex19) xenograft models. Dosing schedules does 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.
  • Synonyms
    ASP8273
  • Pathway
    Angiogenesis
  • Target
    EGFR
  • Recptor
    EGFR
  • Research Area
    Cancer
  • Indication
    Lung Cancer

Chemical Information

  • CAS Number
    1448232-80-1
  • Formula Weight
    562.7063
  • Molecular Formula
    C30H42N8O3
  • Purity
    >98% (HPLC)
  • Solubility
    DMSO
  • 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
  • Chemical Name
    2-Pyrazinecarboxamide, 6-ethyl-3-[[4-[4-(4-methyl-1-piperazinyl)-1-piperidinyl]phenyl]amino]-5-[[(3R)-1-(1-oxo-2-propen-1-yl)-3-pyrrolidinyl]oxy]-

Shipping & Storage Information

  • Storage
    (-20℃)
  • Shipping
    With Ice Pack
  • Stability
    ≥ 2 years

Reference

1. Wang S, et al. J Hematol Oncol. 2016 Apr 12;9:34.
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