Rociletinib
hydrobromide (CO-1686; AVL-301; CNX-419), the hydrobromide salt of Rociletinib, is an oral, irreversible/covalent, and
mutant-selective EGFR inhibitor (EGFR-TKI) with antitumor activity. It inhibits EGFRL858R/T790M and EGFRWT with Ki values of 21.5 nM and 303.3 nM in cell-free assays,
respectively. Rociletinib binds to and inhibits mutant forms of EGFR,
including T790M, thereby leading to cell death of resistant tumor cells.
Compared to other EGFR inhibitors, Rociletinib inhibits T790M, a
secondary acquired resistance mutation, as well as other mutant EGFRs
and may have therapeutic benefits in tumors with T790M-mediated
resistance to other EGFR tyrosine kinase inhibitors.
纯度:≥98%
CAS:1446700-26-0