产品描述:
CNX-2006 is an irreversible inhibitor of mutant EGFRs.{54404} It 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. It is greater than 10-fold selective for cells expressing these mutants over A549 cells expressing wild-type EGFR. CNX-2006 inhibits growth in a panel of non-small cell lung cancer (NSCLC) cells expressing wild-type or mutant EGFRs (GI50s = 0.34-8 and 0.003-3.6 μM, respectively). It reduces tumor growth in an NCI H1975 mouse xenograft model when administered at doses of 25 and 50 mg/kg.