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Pack Size | Price | Availability | Quantity |
---|---|---|---|
2 mg | $58 | 5 days |
Description | Naquotinib mesylate (ASP8273 (mesylate)) is an orally available, mutant-selective and irreversible inhibitor of EGFR(iC50s of 8-33 nM and 230 nM for toward EGFR mutants and EGFR). |
Targets&IC50 | EGFR:230 nM |
In vitro | In NCI-H1650 (del ex19), Naquotinib inhibits cell growth with an IC50 value of 70nM while other EGFR-TKIs are only partially effective.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[2]. |
In vivo | 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]. |
Alias | ASP8273 (mesylate) |
Molecular Weight | 658.81 |
Formula | C31H46N8O6S |
Cas No. | 1448237-05-5 |
Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | ||||||||||||||||||||
Solubility Information | DMSO: 12.5 mg/mL (18.97 mM), Sonication and heating are recommended. | ||||||||||||||||||||
Solution Preparation Table | |||||||||||||||||||||
DMSO
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