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| | Naquotinib Basic information |
| Product Name: | Naquotinib | | Synonyms: | Naquotinib;ASP-8273;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;(R)-5-((1-acryloylpyrrolidin-3-yl)oxy)-6-ethyl-3-((4-(4-(4-methylpiperazin-1-yl)piperidin-1-yl)phenyl)amino)pyrazine-2-carboxamide;Naquotinib,ASP-8273;NAQUOTINIB (FREE BASE);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]-;Epidermal growth factor receptor,EGFR,ASP 8273,HER1,ErbB-1,ASP-8273,inhibit,Naquotinib,Inhibitor | | CAS: | 1448232-80-1 | | MF: | C30H42N8O3 | | MW: | 562.71 | | EINECS: | | | Product Categories: | | | Mol File: | 1448232-80-1.mol |  |
| | Naquotinib Chemical Properties |
| 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) |
| | Naquotinib Usage And Synthesis |
| 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). | | target | |
| | Naquotinib Preparation Products And Raw materials |
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