An active metabolite of AZ 9291
AZ 7550 is an active metabolite of AZ 9291 .1 It inhibits the insulin-like growth factor 1 receptor (IGF-1R) in a cell-free assay (IC50 = 1.6 ?M). It inhibits EGFR autophosphorylation in H1975 and PC-9 cells expressing the respective constitutively active mutants EGFRT790M/L858R and EGFRExon19del (IC50s = 0.045 and 0.026 ?M, respectively), as well as in LoVo cells expressing wild-type EGFR (IC50 = 0.786 ?M).
1.Finlay, M.R., Anderton, M., Ashton, S., et al.Discovery of a potent and selective EGFR inhibitor (AZD9291) of both sensitizing and T790M resistance mutations that spares the wild type form of the receptorJ. Med. Chem.57(20)8249-8267(2014)
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