Naquotinib mesylate
Modify Date: 2025-08-25 06:45:11
Naquotinib mesylate structure
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Common Name | Naquotinib mesylate | ||
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| CAS Number | 1448237-05-5 | Molecular Weight | 658.812 | |
| Density | N/A | Boiling Point | N/A | |
| Molecular Formula | C31H46N8O6S | Melting Point | N/A | |
| MSDS | N/A | Flash Point | N/A | |
Use of Naquotinib mesylateNaquotinib mesylate (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 | Naquotinib mesylate |
|---|---|
| Synonym | More Synonyms |
| Description | Naquotinib mesylate (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 |
EGFRL858R/T790M EGFRL858R EGFRExon 19 deletion EGFRExon 19 deletion/T790M EGFR:230 nM (IC50) |
| 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 |
| Molecular Formula | C31H46N8O6S |
|---|---|
| Molecular Weight | 658.812 |
| Exact Mass | 658.326111 |
| Storage condition | 2-8℃ |
| 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 monomethanesulfonate |
| 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 monomethanesulfonate |
| UNII-12T09LV21O |
| 5-{[(3R)-1-Acryloyl-3-pyrrolidinyl]oxy}-6-ethyl-3-({4-[4-(4-methyl-1-piperazinyl)-1-piperidinyl]phenyl}amino)-2-pyrazinecarboxamide methanesulfonate (1:1) |
| ASP8273 mesilate |
| Naquotinib mesilate |
| Naquotinib mesylate |
| 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]-, methanesulfonate (1:1) |
| 12T09LV21O |
| Naquotinib (mesylate) |