Avitinib

Research use only, not for human use.

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

Avitinib (AC-0010, AC0010) is an orally available, irreversible, and mutant-selective EGFR inhibitor with IC50 of 0.18 nM against EGFR L858R/T790M; displays 43-fold greater potency over wild-type EGFR (IC50=7.68 nM); 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; overcomes T790M-induced resistance in animal models and lung cancer patients without hyperglycemia or other severe adverse effects.Lung Cancer Phase 2 Clinical

AC-0010;AC0010

Angiogenesis

EGFR

EGFR

Cancer

Lung Cancer

1557267-42-1

487.54

C26H26FN7O2

>98% (HPLC)

DMSO: 88 mg/mL (180.5 mM) （ < 1 mg/ml refers to the product slightly soluble or insoluble )

C=CC(NC1=CC=CC(OC2=C3C(NC=C3)=NC(NC4=CC=C(N5CCN(C)CC5)C(F)=C4)=N2)=C1)=O

N-[3-[[2-[[3-Fluoro-4-(4-methyl-1-piperazinyl)phenyl]amino]-7H-pyrrolo[2,3-d]pyrimidin-4-yl]oxy]phenyl]-2-propenamide

(-20℃)

With Ice Pack

≥ 2 years