Osimertinib | Mutant EGFR kinase inhibitor

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Osimertinib (1421373-65-0) 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

References/Citations:

  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
1421373-65-0, AZD9291, egfr inhibitor, EGFR Kinase Inhibitor, mutant egfr kinase inhibitor, osimertinib, Osimertinib supplier, T790M mutant inhibitor
Alternate Name:
AZD9291

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Materials provided by Focus Biomolecules are for laboratory research use only and are not intended for human or veterinary applications. Please note that we do not sell to individuals and that all orders placed by non-research organizations will incur a $20 restocking/refund fee

Osimertinib (1421373-65-0) 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

References/Citations:

  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