| Identification | Back Directory | [Name]
Naquotinib | [CAS]
1448232-80-1 | [Synonyms]
ASP-8273
Naquotinib
Naquotinib,ASP-8273
NAQUOTINIB (FREE BASE)
(R)-5-((1-acryloylpyrrolidin-3-yl)oxy)-6-ethyl-3-((4-(4-(4-methylpiperazin-1-yl)piperidin-1-yl)phenyl)amino)pyrazine-2-carboxamide
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]-2-pyrazinecarboxamide
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]- | [Molecular Formula]
C30H42N8O3 | [MDL Number]
MFCD30496701 | [MOL File]
1448232-80-1.mol | [Molecular Weight]
562.71 |
| Chemical Properties | Back Directory | [Boiling point ]
717.6±60.0 °C(Predicted) | [density ]
1.248±0.06 g/cm3(Predicted) | [storage temp. ]
Store at -20°C | [solubility ]
DMF: 30mg/ml; DMSO: 2 mg/ml; Ethanol: 30mg/ml | [form ]
A crystalline solid | [pka]
14.10±0.50(Predicted) | [color ]
Light yellow to yellow |
| Hazard Information | Back Directory | [Uses]
Naquotinib is an epidermal growth factor receptor (EGFR) inhibitor. | [Biological Activity]
Naquotinib (ASP8273) is an orally active, irreversible, mutant-selective epidermal growth factor receptor (EGFR) inhibitor with potential antitumor activity. | [in vitro]
ASP8273 is an irreversible TKI small molecule inhibitor that inhibits the kinase activity of EGFR mutants including T97M with limited activity against wild-type EGFR. In in vitro enzymatic activity and cellular assays, ASP8273 covalently bound to an EGFR mutant (L858R/T790M) through cysteine residues and long-term inhibited EGFR phosphorylation for 24 hours. In NSCLC cell lines with the above-mentioned EGFR mutations, ASP8273 has IC50 values in the range of 8-33 nM for EGFR mutants, more potent than WT EGFR (IC50 for WT EGFR is 230 nM). | [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[2]. | [target]
| [IC 50]
EGFR: 230 nM (IC50); EGFRT790M; EGFRL858R/T790M; EGFRL858R; EGFRExon 19 deletion/T790M |
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