Naquotinib structure
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Common Name | Naquotinib | ||
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CAS Number | 1448232-80-1 | Molecular Weight | 562.706 | |
Density | 1.2±0.1 g/cm3 | Boiling Point | 717.6±60.0 °C at 760 mmHg | |
Molecular Formula | C30H42N8O3 | Melting Point | N/A | |
MSDS | N/A | Flash Point | 387.8±32.9 °C |
Use of NaquotinibNaquotinib (ASP8273) is an orally available, mutant-selective and irreversible EGFR inhibitor; with IC50s of 8-33 nM toward EGFR mutants and 230 nM for EGFR. |
Name | 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 |
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Synonym | More Synonyms |
Description | Naquotinib (ASP8273) is an orally available, mutant-selective and irreversible EGFR inhibitor; with IC50s of 8-33 nM toward EGFR mutants and 230 nM for EGFR. |
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Related Catalog | |
Target |
EGFR:230 nM (IC50) EGFRT790M EGFRL858R/T790M EGFRL858R EGFRExon 19 deletion/T790M |
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[1]. 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[2]. |
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]. |
References |
Density | 1.2±0.1 g/cm3 |
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Boiling Point | 717.6±60.0 °C at 760 mmHg |
Molecular Formula | C30H42N8O3 |
Molecular Weight | 562.706 |
Flash Point | 387.8±32.9 °C |
Exact Mass | 562.338013 |
LogP | 3.74 |
Vapour Pressure | 0.0±2.3 mmHg at 25°C |
Index of Refraction | 1.624 |
Storage condition | -20℃ |
Naquotinib |
6-Ethyl-3-{4-[4-(4-methylpiperazin-1-yl)piperidin-1-yl]anilino}-5-{[(3R)-1-(prop-2-enoyl)pyrrolidin-3-yl]oxy}pyrazine-2-carboxamide |
UNII-47DD4548PB |
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]- |
ASP8273 |
5-{[(3R)-1-Acryloyl-3-pyrrolidinyl]oxy}-6-ethyl-3-({4-[4-(4-methyl-1-piperazinyl)-1-piperidinyl]phenyl}amino)-2-pyrazinecarboxamide |
6-ethyl-3-({4-[4-(4-methylpiperazin-1-yl)piperidin-1-yl]phenyl}amino)-5-{[(3R)-1-(1-oxoprop-2-en-1-yl)pyrrolidin-3-yl]oxy}pyrazine-2-carboxamide |