Cayman Bms 986205; Size- 5 Mg

CNX-2006 is an irreversible inhibitor of mutant EGFRs. It inhibits EGFR phosphorylation in PC-9 and HCC827 cells (IC₅₀s = 55-104 nM), which express the EGFR^{Del E746_A750} mutation, and NCI H1975 and PC-9/GR4 cells (IC₅₀s = 46 and 61 nM, respectively), which express the EGFR^L858R/T790M and EGFR^{Del 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.

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