AZD3759 (Synonyms: AZD3759) |
Catalog No.GC13143 |
AZD3759 (AZD3759) es un inhibidor de EGFR potente, activo por vÍa oral, que penetra en el sistema nervioso central. En concentraciones de Km ATP, las IC50 son 0,3, 0,2 y 0,2 nM para EGFRwt, EGFRL858R y EGFRexon 19Del, respectivamente.
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Cas No.: 1626387-80-1
Sample solution is provided at 25 µL, 10mM.
AZD3759 is a potent and oral active inhibitor of EGFR (IC50= 7.0-7.7 nM) with antineoplastic activity.
EGFR (epidermal growth factor receptor) is a cell-surface receptor tyrosine kinase. The receptor activation leads to dimerization and tyrosine autophosphorylation. It induces a cascade of downstream cellular responses such as modification in gene expression, cell proliferation and cytoskeletal rearrangement etc.
AZD3759 shows equally potent inhibitory effect on cell phosphorylation or proliferation in EGFR-activating mutant cell lines (PC-9 and H3255) in the range of 7.0−7.7nM. In cellular phosphorylation assays, AZD3759 also exhibits 9-fold inhibition selectivity in EGFR-activating
mutant cell lines over EGFR wild-type cell lines (H838). [1]
In brain metastasis mouse model, AZD3759 demonstrates prominent antitumor efficacy in a dose dependent manner (∼78% tumor growth inhibition at 7.5 mg/kg qd and tumor regression at 15 mg/kg qd, respectively, 4 weeks after treatment, with <20% body weight loss). In addition, at the doses of 7.5 and 15 mg/k, AZD3759 significantly decreases tumor area in the brain tissue collected from the same mouse model. [1]
Reference:
Zeng Q, Wang J, Cheng Z et al. Discovery and Evaluation of Clinical Candidate AZD3759, a Potent, Oral Active, Central Nervous System-Penetrant, Epidermal Growth Factor Receptor Tyrosine Kinase Inhibitor. J Med Chem. 2015 Oct 22;58(20):8200-15
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