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Osimertinib (mesylate)
$60 – $190
Products Details
Product Description
– Osimertinib mesylate (AZD9291 mesylate) 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. Osimertinib overcomes T790M-mediated resistance to EGFR inhibitors in lung cancer[1].
Web ID
– HY-15772A
Storage Temperature
– 4°C (Powder, sealed storage, away from moisture)
Shipping
– Room Temperature
Applications
– Cancer-Kinase/protease
Molecular Formula
– C29H37N7O5S
Citations
– Cancer Cell. 2020 Jan 13;37(1):104-122.e12.|Cancer Lett. 2023 May 19;216237.|Oncotarget. 2017 Dec 6;9(2):1641-1655.|Research Square Preprint. 2023 Jun 30.|Xenobiotica. 2018 Nov;48(11):1106-1112.|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.|Am J Cancer Res. 2023 Sep 15;13(9):4145-4162.|Am J Transl Res. 2021 Jun 15;13(6):6055-6065.|Anticancer Res. 2019 Sep;39(9):4817-4828.|Bioorg Chem. 2023 Mar 27.|bioRxiv. 2023 Oct 27.|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 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 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.|Commun Biol. 2021 Dec 13;4(1):1391.|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.|Faculty of Medicine. University of Oslo. 2019 Feb.|Fundam Clin Pharmacol. 2021 Feb 1.|Genes Cancer. 2017 Mar;8(3-4):497-504.|Int Immunopharmacol. 2023 Nov 23:126:111265.|Int J Anal Chem. 2020 Dec 29.|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 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 Ther. 2018 Mar;17(3):603-613.|Mol Cancer Ther. 2019 May;18(5):920-928.|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.|Oncogene. 2022 May;41(22):3104-3117.|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.|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 Print. December 21st, 2022.|Respir Physiol Neurobiol. 2020 Oct;281:103496.|RSC Chem Biol. 2023 Aug 29.|Theranostics. 2021 Jan 19;11(7):3392-3416.|Theranostics. 2021 Mar 24;11(12):5650-5674.|Universitat Politècnica de València. 2021 Sep.|Research Square Preprint. 2021 May.
References
– [1][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.|[2]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.
CAS Number
– 1421373-66-1
Molecular Weight
– 595.71
Compound Purity
– 99.96
SMILES
– C=CC(NC1=CC(NC2=NC=CC(C3=CN(C)C4=C3C=CC=C4)=N2)=C(OC)C=C1N(CCN(C)C)C)=O.CS(=O)(O)=O
Clinical Information
– Launched
Research Area
– Cancer
Solubility
– DMSO : 13.89 mg/mL (ultrasonic;warming;heat to 80°C)
Target
– EGFR
Isoform
– EGFR/ErbB1/HER1
Pathway
– JAK/STAT Signaling;Protein Tyrosine Kinase/RTK
Product type
– Reference compound
Disclaimer: All products are for Research use only unless clearly stated otherwise on the product datasheet. Datasheets provided on the website are drafts for reference purpose only and you are requested to always refer to the hard copy included in the kit for your experimentation. Agdia Products are available for delivery only in Canada.
