产品描述:
AZ 5104 is an inhibitor of mutant EGFRs (IC50 = 2 nM for EGFRL858R/T790M and EGFRT790M for both) and an active metabolite of AZD 9291 (Item No. 16237).{27820} It is selective for these mutant EGFRs over wild-type EGFR (IC50 = 33 nM). AZ 5104 is formed from AZD 9291 by the cytochrome P450 (CYP) isoform CYP3A.{32544} It decreases proliferation of H1975 non-small cell lung cancer (NSCLC) cells containing the L858R activating and T790M resistance mutations (GI50 = 24 nM). AZ 5104 (2.5-10 mg/kg per day) reduces tumor growth in an H1975 mouse xenograft model.