Osimertinib
Mutant EGFR kinase inhibitor / Osimertinib is a potent, selective, irreversible inhibitor of mutant EFGR tyrosine kinase.1 Osimertinib inhibits phosphorylation of EGFR in T790M-mutant cell lines (IC50 <15 nM) but was less potent at inhibition of EGFR phosphorylation in wild-type cells (IC50s in the range of 480 to 1,865 nM). It produces sustained tumor regression in EGFR-mutant tumor xenograft and transgenic rodent models.2 Tumor cells develop resistance to osimertinib but combination treatment with an IL-6 antibody reverses resistance to a certain extent.3 In clinical use for treatment of non-small cell lung cancer.4
Biochemicals & reagents
1421373-65-0
AZD-9291
1 Finlay et al. (2014), Discovery of a potent and selective EGFR inhibitor (AZD9291) of both sensitizing and T790M resistance mutations that spares the wild type form of the receptor; J. Med. Chem., 57 8249 2 Cross et al. (2014), AZD9291, an irreversible EGFR TKI, overcomes T790M-mediated resistance to EGFR inhibitors in lung cancer; Cancer Discov., 4 1046 3 Tan et al. (2024), Evaluation of drug resistance for EGFR-TKIs in lung cancer via multicellular lung-on-a-chip; Eur. J. Pharm. Sci., 199 106805 4 Patel et al. (2017); Recent updates on third generation EGFR inhibitors and emergence of fourth generation EGFR inhibitors to combat C797S resistance; J. Med. Chem., 142 32
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TARGET: Kinase -- PATHWAY: EGF -- DISEASE AREA: Cancer