Description:
Almonertinib (HS10296) is a novel, potent, orally
bioavailable, 3rd-generation irreversible inhibitor of the epidermal
growth factor receptor (EGFR) mutant form T790M, with potential
antineoplastic activity. HS-10296 binds to and inhibits EGFR T790M, a
secondarily acquired resistance mutation, inhibits the tyrosine kinase
activity of EGFR T790M, prevents EGFR T790M-mediated signaling and leads
to cell death in EGFR T790M-expressing tumor cells. EGFR, a receptor
tyrosine kinase that is mutated in many tumor cell types, plays a key
role in tumor cell proliferation and tumor vascularization.
References:
[1]. Sullivan
I, et al. Next-Generation EGFR Tyrosine Kinase Inhibitors for Treating
EGFR-Mutant Lung Cancer beyond First Line. Front Med (Lausanne). 2017
Jan 18;3:76.
[2]. Wu
SG, et al. Management of acquired resistance to EGFR TKI-targeted
therapy in advanced non-small cell lung cancer. Mol Cancer. 2018 Feb
19;17(1):38.
Related CAS No: 1899921-05-1 (free base); 2134096-03-8 (HCl)