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Naquotinib mesylate

Chemical Structure : Naquotinib mesylate

CAS No.: 1448237-05-5

Naquotinib mesylate (ASP-8273, ASP8273)

Catalog No.: PC-45722Not For Human Use, Lab Use Only.

Naquotinib (ASP-8273) is a potent, irreversible, mutant-selective inhibitor of EGFR (IC50=8-33 nM for (L858R, exon 19 deletion, L858R/T790M, and del19/T790M)).

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Purity & Documentation Purity: >98% (HPLC) Select Batch:

Biological Activity

Naquotinib (ASP-8273) mesylateis a potent, irreversible, mutant-selective inhibitor of EGFR (IC50=8-33 nM for (L858R, exon 19 deletion, L858R/T790M, and del19/T790M)).
Naquotinib (ASP-8273) is more potently than that of WT EGFR (IC50= 230 nM).
Naquotinib (ASP-8273) shows activity in mutant EGFR cell line which is resistant to other EGFR TKIs including AZD9291 and CO-1686.

Physicochemical Properties

M.Wt 658.812
Formula C31H46N8O6S
Appearance Solid
CAS No.
Storage
Solide Powder
-20 °C 12 Months; 4°C 6 Months
In Solvent
-80 °C 6 Months; -20°C 6 Months
Shipping
Solubility

DMSO: 12.5 mg/mL

Chemical Name/SMILES

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)

References

1. Wang S, et al. J Hematol Oncol. 2016 Apr 12;9:34.

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