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Avitinib maleate

Chemical Structure : Avitinib maleate

CAS No.: 1557268-88-8

Avitinib maleate (AC-0010MA, AC0010 maleate)

Catalog No.: PC-61450Not For Human Use, Lab Use Only.

Avitinib maleate (AC-0010MA, AC0010 maleate) is an orally available, irreversible, and mutant-selective EGFR inhibitor with IC50 of 0.18 nM against EGFR L858R/T790M.

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Biological Activity

Avitinib maleate (AC-0010MA, AC0010 maleate) is an orally available, irreversible, and mutant-selective EGFR inhibitor with IC50 of 0.18 nM against EGFR L858R/T790M.
Avitinib displays 43-fold greater potency over wild-type EGFR (IC50=7.68 nM).
Avitinib selectively inhibits mutant EGFR phosphorylation (IC50 =7.3 nM and 2.8 nM) in NCI-H1975 and NIH/3T3_TC32T8 cells, 115- and 298-fold more sensitive than that of the inhibition of wild type EGFR in A431.
Avitinib overcomes T790M-induced resistance in animal models and lung cancer patients without hyperglycemia or other severe adverse effects.

Physicochemical Properties

M.Wt 603.611
Formula C30H30FN7O6
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

10 mM in DMSO

Chemical Name/SMILES

N-(3-((2-((3-fluoro-4-(4-methylpiperazin-1-yl)phenyl)amino)-7H-pyrrolo[2,3-d]pyrimidin-4-yl)oxy)phenyl)acrylamide maleate

References

1. Xu X, et al. Mol Cancer Ther. 2016 Nov;15(11):2586-2597.

2. Wang W, et al. J Pharm Biomed Anal. 2017 May 30;139:205-214.

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