Chemical Structure : Avitinib maleate
货号: 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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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
分子量 | 603.611 | |
分子式 | C30H30FN7O6 | |
外观性状 | Solid | |
储存条件 |
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Solubility |
10 mM in DMSO |
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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