Potent, orally active, brain-penetrant, EGFR tyrosine kinase inhibitor (IC50 value 7.2 nM for inhibition of cellular phosphorylation on L858R cell lines), that shows tumor regression in the mouse model with brain metastasis. At 1 µM, AZD3759 showed less than 50% inhibition against 115 out of a panel of 124 recombinant protein and lipid kinases, and was neither a direct inhibitor nor a time-dependent inhibitor for a series of Cytochrome isoforms, suggesting a low enzyme induction liability.

KEYWORDS: AZD3759 | supplier | EGFR inhibitor | AZD-3759 | AZD 3759 | CAS [1626387-80-1] | [1626387-81-2] | EGF | EGFR | Inhibitor | orally active | brain-penetrant | RTK | CNS | tumor regression | metastases | clinical trial | central nervous system