Molecular Weight: 499.607 (or 499.619, with slight variations from different sources)
Physical and Chemical Properties
Density: Approximately 1.2±0.1 g/cm³ (or predicted at 1.19±0.1 g/cm³)
Refractive Index: 1.618
PSA (Polar Surface Area): 87.55000
LogP (Partition Coefficient): 3.30 (or predicted at 4.65580)
Chemical Characteristics
Osimertinib (AZD-9291) is an irreversible and mutant-selective inhibitor of EGFR (Epidermal Growth Factor Receptor). It effectively inhibits the activity of both EGFRL858R and EGFRL858R/T790M mutants, with IC50 values of 12 nM and 1 nM, respectively.
This drug exhibits oral activity and a higher selective inhibition against mutant EGFR compared to wild-type EGFR.
Biological Activity and Uses
Osimertinib is primarily used in the field of cancer treatment, particularly for patients with EGFR-mutated non-small cell lung cancer (NSCLC). It addresses the resistance to EGFR inhibitors mediated by the T790M mutation.
In both in vitro and in vivo studies, Osimertinib has demonstrated significant antitumor activity. For instance, in tumor-bearing mouse models, Osimertinib causes marked tumor regression and inhibits EGFR phosphorylation and its downstream signaling pathways (such as AKT and ERK).
