Description
An irreversible inhibitor of mutant EGFRs; inhibits EGFR phosphorylation in PC-9 and HCC827 cells (IC50s = 55-104 nM), which express the EGFRDel E746_A750 mutation, and NCI H1975 and PC-9/GR4 cells (IC50s = 46 and 61 nM, respectively), which express the EGFRL858R/T790M and EGFRDel E746_A750/T790M mutations, respectively; >10-fold selective for cells expressing these mutants over A549 cells expressing wild-type EGFR; inhibits growth in a panel of NSCLC cells expressing wild-type or mutant EGFRs (GI50s = 0.34-8 and 0.003-3.6 μM, respectively); reduces tumor growth in an NCI H1975 mouse xenograft model at 25 and 50 mg/kg
Formal name: N-[3-[[2-[[4-[[1-(2-fluoroethyl)-3-azetidinyl]amino]-2-methoxyphenyl]amino]-5-(trifluoromethyl)-4-pyrimidinyl]amino]phenyl]-2-propenamide
Synonyms:
Molecular weight: 545.5
CAS: 1375465-09-0
Purity: ≥98%
Formulation: A crystalline solid
