Avitinib maleate

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

阿维替尼马来酸盐（AC-0010MA、AC0010马来酸盐）是一种口服、不可逆、突变选择性 EGFR 抑制剂，针对 EGFR L858R/T790M 的 IC50 为 0.18 nM。

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; 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.

Western Blot Analysis Cell Line:NCI-H1975, HCC827, A431 cells Concentration:0.13 nM, 0.64 nM, 3.2 nM, 16 nM, 80 nM, 0.4 μM, 2 μM Incubation Time:2 h Result:Selectively inhibits mutant EGFR phosphorylation with IC50 values of 7.3 and 2.8 nM in NCI-H1975 and NIH/3T3_TC32T8 cells.

Animal Model:Nu/Nu nude mice (Six- to 8-week-old) injected with NCI-H1975 and A431 cells Dosage:12.5, 50, and 500 mg/kg Administration:Orally administration; once daily; for 14 days Result:Inhibited EGFR-mutant tumor growth but not wild-type EGFR tumor growth.

AC-0010MA | AC0010 maleate

Angiogenesis

EGFR

EGFR

Cancer

Lung Cancer

1557268-88-8

603.611

C30H30FN7O6

>98% (HPLC)

DMSO : ≥ 300 mg/mL 497.02 mM

CN1CCN(CC1)C2=C(C=C(C=C2)NC3=NC4=C(C=CN4)C(=N3)OC5=CC=CC(=C5)NC(=O)C=C)F.C(=CC(=O)O)C(=O)O

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

(-20℃)

With Ice Pack

≥ 2 years