Mutated EGFR-IN-2

Mutated EGFR-IN-2 (compound 91) is a mutant-selective EGFR inhibitor extracted from patent WO2017036263A1, which potently inhibits single-mutant EGFR (T790M) and double-mutant EGFR (including L858R/T790M (IC50=＜1nM) and ex19del/T790M), and can suppress activity of single gain-of-function mutant EGFR (including L858R and ex19del) as well. Mutated EGFR-IN-2 shows anti-tumor antivity[1].

Research Areas >> Cancer

Signaling Pathways >> JAK/STAT Signaling >> EGFR

Signaling Pathways >> Protein Tyrosine Kinase/RTK >> EGFR

EGFRT790M

EGFRL858R

EGFRex19del

EGFR (L858R/T790M):<1 nM (IC50)

EGFR (ex19del/T790M)

[1]. 2, 4-di-(nitrogen containing group) substituted pyrimidine compound and preparation method and use thereof.