Description
An inhibitor of mutant EGFRs (IC50s = 2-2,740 nM); selective for EGFR mutants including EGFRL858R and EGFRDel E746_A750 (IC50s = 2 nM for both) over wild-type EGFR (IC50 = 750 nM); inhibits ERBB2Ins G776V,C and wild-type ERBB2 (IC50s = 10 and 24 nM, respectively, in Ba/F3 cells) but not the ERBB2 gatekeeper mutant; decreases phosphorylation of EGFR, AKT, and ERK1/2 in H1975 NSCLC cells at 10-1,000 nM; inhibits proliferation of PC-9 and PC-9 GR cells (EC50s = 15 and 3 nM, respectively)
Formal name: N-[3-[[5-chloro-2-[[4-(4-methyl-1-piperazinyl)phenyl]amino]-4-pyrimidinyl]oxy]phenyl]-2-propenamide
Synonyms:
Molecular weight: 465
CAS: 1214265-56-1
Purity: ≥98%
Formulation: A crystalline solid
Product Type|Biochemicals|Kinase Inhibitors|EGFR/ErbB/HER Family||Product Type|Biochemicals|Small Molecule Inhibitors|Kinases||Research Area|Cancer|Cell Signaling|Growth Factor Receptor Signaling
