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Avitinib

Chemical Structure : Avitinib

CAS No.: 1557267-42-1

Avitinib (Abivertinib;AC-0010;AC0010)

Catalog No.: PC-61449Not For Human Use, Lab Use Only.

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

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

Biological Activity

Avitinib (Abivertinib, AC-0010, AC0010) is an orally available, irreversible, and mutant-selective EGFR inhibitor with IC50 of 0.18 nM against EGFR L858R/T790M.
Avitinib (Abivertinib, AC-0010) displays 43-fold greater potency over wild-type EGFR (IC50=7.68 nM).
Avitinib (Abivertinib, AC-0010) 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 (Abivertinib, AC-0010) overcomes T790M-induced resistance in animal models and lung cancer patients without hyperglycemia or other severe adverse effects.

Physicochemical Properties

M.Wt 487.539
Formula C26H26FN7O2
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-methyl-1-piperazinyl)phenyl]amino]-7H-pyrrolo[2,3-d]pyrimidin-4-yl]oxy]phenyl]-2-propenamide

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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