Product Description: Osimertinib (AZD9291) is a covalent, orally active, irreversible, and mutant-selective EGFR inhibitor with an apparent IC50 of 12 nM against L858R and 1 nM against L858R/T790M, respectively. Osimertinib overcomes T790M-mediated resistance to EGFR inhibitors in lung cancer[1].
Applications: Cancer-Kinase/protease
Formula: C28H33N7O2
Citations: ACS Nano. 2022 Jul 21./Acta Pharmacol Sin. 2019 Dec;40(12):1587-1595. /Acta Pharmacol Sin. 2021 Jan 7./Acta Pharmacol Sin. 2021 Jan;42(1):108-114./Acta Pharmacol Sin. 2024 Dec 3./Adv Sci (Weinh). 2024 Dec 16:e2411479./Adv Sci (Weinh). 2024 May 2:e2306348./Adv Ther. 2024 Jul 18./Am J Cancer Res. 2023 Sep 15;13(9):4145-4162./Am J Transl Res. 2021 Jun 15;13(6):6055-6065./Anticancer Res. 2024 Oct;44(10):4175-4188./Anticancer Res. 2019 Sep;39(9):4817-4828./Appl Surf Sci. 2024 Dec 21./Biochem Biophys Res Commun. 2024 Sep 19:733:150711./Biomed Pharmacother. 2024 Jan 9:171:116124./Bioorg Chem. 2023 Mar 27./bioRxiv. 2023 Oct 27./bioRxiv. 2024 Feb 12./Cancer Cell Int. 2021 Apr 15;21(1):216./Cancer Cell Int. 2021 Jul 3;21(1):337./Cancer Discov. 2019 Jul;9(7):926-943./Cancer Gene Ther. 2022 Sep 19./Cancer Res Treat. 2023 Jan 26./Cancer Res. 2023 Apr 16;CAN-22-3059./Cancer Res. 2023 Dec 14./Cancer Res. 2023 May 2;83(9):1490-1502./Cancers. 2019 Jul 5;11(7):947./Cancers. 2019 Oct 14;11(10):1550./Cell Chem Biol. 2018 Aug 16;25(8):996-1005.e4./Cell Death Differ. 2024 May 30./Cell Death Dis. 2019 Aug 13;10(8):615./Cell Death Dis. 2019 May 1;10(5):361. /Cell Oncol. 2022 Sep 21./Cell Rep Med. 2023 Jan 10;100911./Cell Rep Med. 2024 Mar 19;5(3):101471./Cell Rep. 2024 Oct 8;43(10):114812./Commun Biol. 2021 Dec 13;4(1):1391./Cytotechnology. 2025 Feb;77(1):23./Drug Deliv Transl Res. 2021 Nov 23./Drug Metab Pharmacokinet. 2020 Oct;35(5):456-465./Environ Toxicol. 2019 Apr;34(4):476-485. /Eur J Drug Metab Pharmacokinet. 2021 Jul 18;1-11./Eur J Pharmacol. 2021, 174297./Exp Hematol Oncol. 2024 Oct 1;13(1):97./Faculty of Medicine. University of Oslo. 2019 Feb./Fundam Clin Pharmacol. 2021 Feb 1./Genes (Basel). 2024 Dec 19;15(12):1624./Genes Cancer. 2017 Mar;8(3-4):497-504./Genes Genomics. 2024 Dec 20./Int Immunopharmacol. 2023 Nov 23:126:111265./Int J Anal Chem. 2020 Dec 29./Int J Biol Macromol. 2024 May;268(Pt 1):131560./Int J Biol Sci. 2021; 17(7):1671-1681./Int J Mol Med. 2023 Nov;52(5):102./Int J Mol Sci. 2023 May 15, 24(10), 8794./Int J Oncol. 2020 Jan;56(1):243-257./J Biol Chem. 2023 May 11;104814./J Cell Physiol. 2021 Nov 21./J Chromatogr B Analyt Technol Biomed Life Sci. 2024 Mar 26:1237:124100./J Control Release. 2024 Nov 5:376:829-841./J Ethnopharmacol. 2024 Jul 18:118586./J Exp Clin Cancer Res. 2019 Mar 15;38(1):129./J Exp Clin Cancer Res. 2019 Mar 15;38(1):129. /J Exp Clin Cancer Res. 2019 May 23;38(1):219. /J Med Chem. 2017 Apr 13;60(7):2944-2962. /J Med Chem. 2023 Apr 11./J Nat Med. 2023 Apr 12./J Natl Cancer Inst. 2023 Jul 22;djad142./J Pharm Anal. 2021 Jun 19./Mol Cancer Res. 2019 Feb;17(2):499-507. /Mol Cancer Res. 2019 Nov;17(11):2233-2243./Mol Cancer Res. 2024 Jul 2./Mol Cancer Ther. 2018 Mar;17(3):603-613./Mol Cancer Ther. 2019 May;18(5):920-928./Mol Cancer Ther. 2023 Sep 5;22(9):1013-1027./Mol Med Rep. 2021 Jan;23(1):48./Mol Oncol. 2023 Apr 4./Mol Pharmacol. April 5, 2022./Nat Cancer. 2022 Apr;3(4):402-417./Nat Cancer. 2023 Jun;4(6):829-843./Neoplasia. 2024 Aug 14:57:101039./Oncogene. 2022 May;41(22):3104-3117./Oncogene. 2024 Aug 15./Oncogene. 2024 Oct 14./Oncol Lett. 2023 Jul 20./Oncotarget. 2015 Oct 13;6(31):31313-22. /Oncotarget. 2016 Oct 25;7(43):69760-69769./Oncotarget. 2017 Mar 14;8(11):18359-18372. /Patent. US20190010159A1./Patent. US20200276189A1./Patent. US20210315911A1./Patent. US20230158019A1./Pharmaceutics. 2024 Nov 12;16(11):1444./Research Square Preprint. 2021 Jul./Research Square Preprint. 2021 Jun./Research Square Preprint. 2021 Mar./Research Square Preprint. 2021 May./Research Square Preprint. 2023 May 5./Research Square Preprint. 2024 Dec 02./Research Square Preprint. 2024 Jan 3./Research Square Preprint. 2024 Nov 26./Research Square Print. December 21st, 2022./Respir Physiol Neurobiol. 2020 Oct;281:103496./Respir Res. 2024 May 20;25(1):215./RSC Chem Biol. 2023 Aug 29./Theranostics. 2021 Jan 19;11(7):3392-3416./Theranostics. 2021 Mar 24;11(12):5650-5674./Transl Lung Cancer Res. 2024 Oct 31;13(10):2698-2712./Universitat Politècnica de València. 2021 Sep./Cancer Cell. 2020 Jan 13;37(1):104-122.e12./Cancer Lett. 2023 May 19;216237./Commun Biol. 2024 Mar 1;7(1):250./Int J Electrochem Sci. 2024 Nov 26./Oncotarget. 2017 Dec 6;9(2):1641-1655./Research Square Preprint. 2023 Jun 30./Xenobiotica. 2018 Nov;48(11):1106-1112./Research Square Preprint. 2021 May.
References: [1]Cross DA, et al. AZD9291, an irreversible EGFR TKI, overcomes T790M-mediated resistance to EGFR inhibitors in lung cancer. Cancer Discov. 2014 Sep;4(9):1046-61./[2]Hirano T, et al. Pharmacological and Structural Characterizations of Naquotinib, a Novel Third-Generation EGFR Tyrosine Kinase Inhibitor, in EGFR-Mutated Non-Small Cell Lung Cancer. Mol Cancer Ther. 2018 Apr;17(4):740-750.
CAS Number: 1421373-65-0
Molecular Weight: 499.61
Compound Purity: 99.99
Research Area: Cancer
Solubility: DMSO : 100 mg/mL (ultrasonic)
Target: EGFR