Osimertinib mesylate
Based on 194 publication(s) in Google Scholar
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.
For research use only. We do not sell to patients.
- Purity: 99.97%
- CAS No.: 1421373-66-1
- Formula: C29H37N7O5S
- Molecular Weight:595.71
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Storage:
4°C, sealed storage, away from moisture
* In solvent : -80°C, 2 years; -20°C, 1 year (sealed storage, away from moisture)
Publications Citing Use of MedChemExpress (MCE) Osimertinib mesylate
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- Nat Commun. 2026 Feb 24;17(1):3113. [Abstract]
- Nat Commun. 2026 Jan 21;17(1):1902. [Abstract]
- Cell Death Differ. 2024 Sep;31(9):1140-1156. [Abstract]
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- Adv Sci (Weinh). 2025 Jun 23:e03322. [Abstract]
- Adv Sci (Weinh). 2024 Dec 16:e2411479. [Abstract]
- Adv Sci (Weinh). 2024 Jul;11(26):e2306348. [Abstract]
- Exp Hematol Oncol. 2024 Oct 1;13(1):97. [Abstract]
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- Respir Res. 2024 May 20;25(1):215. [Abstract]
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- Mol Cancer Res. 2024 Nov 1;22(11):1051-1063. [Abstract]
- Int Immunopharmacol. 2024 Jan 5:126:111265. [Abstract]
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- Eur J Pharmacol. 2021 Sep 15:907:174297. [Abstract]
- Mol Cancer Res. 2019 Nov;17(11):2233-2243. [Abstract]
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- Cell Rep Methods. 2026 Jun 15;6(6):101339. [Abstract]
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- Mol Oncol. 2023 Aug;17(8):1648-1665. [Abstract]
- Cancers. 2019 Oct 14;11(10):1550. [Abstract]
- Cancers. 2019 Jul 5;11(7):947. [Abstract]
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- J Cell Physiol. 2022 Mar;237(3):1780-1789. [Abstract]
- Sci Rep. 2026 Mar 20;16(1):14300. [Abstract]
- J Biol Chem. 2023 Jun;299(6):104814. [Abstract]
- Cancer Res Treat. 2023 Jul;55(3):778-803. [Abstract]
- Bioengineering (Basel). 2025 Oct 19;12(10):1121. [Abstract]
- Transl Lung Cancer Res. 2025 Jun 30;14(6):2159-2179. [Abstract]
- Transl Lung Cancer Res. 2024 Oct 31;13(10):2698-2712. [Abstract]
- Mol Med Rep. 2021 Jan;23(1):48. [Abstract]
- BMC Cancer. 2025 Apr 8;25(1):641. [Abstract]
- Toxicol Appl Pharmacol. 2025 Apr 3:117327. [Abstract]
- Cancer Res Commun. 2026 Mar 10. [Abstract]
- Basic Clin Pharmacol Toxicol. 2025 Dec;137(6):e70143. [Abstract]
- Environ Toxicol. 2019 Apr;34(4):476-485. [Abstract]
- Front Biosci (Landmark Ed). 2025 Sep 25;30(9):40454. [Abstract]
- RSC Chem Biol. 2023 Aug 29;4(11):894-905. [Abstract]
- Mol Pharmacol. 2022 Jun;101(6):381-389. [Abstract]
- Discov Oncol. 2025 Aug 12;16(1):1541. [Abstract]
- Am J Cancer Res. 2023 Sep 15;13(9):4145-4162. [Abstract]
- Genes (Basel). 2024 Dec 19;15(12):1624. [Abstract]
- J Chromatogr B Analyt Technol Biomed Life Sci. 2024 Apr 15:1237:124100. [Abstract]
- PLoS One. 2024 Nov 1;19(11):e0308647. [Abstract]
- World J Gastrointest Oncol. 2025 Aug 15;17(8):108535. [Abstract]
- J Nat Med. 2023 Jun;77(3):523-534. [Abstract]
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- Int J Anal Chem. 2020 Dec 28:2020:8814214. [Abstract]
- Anticancer Res. 2019 Sep;39(9):4817-4828. [Abstract]
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- Biol Methods Protoc. 2025 Feb 13;10(1):bpaf012. [Abstract]
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IF
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IF
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WB
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Cell Proliferation/Viability Assay
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WB
All EGFR Isoforms
More
Biological Activity
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EGFRL858R/T790M 1 nM (IC50) |
EGFRL858R 12 nM (IC50) |
Osimertinib (AZD-9291) shows similar potency to early generation tyrosine kinase inhibitor (TKIs) in inhibiting EGFR phosphorylation in EGFR cells harboring sensitising EGFR mutants including PC-9 (ex19del), H3255 (L858R) and H1650 (ex19del), with mean IC50 values ranging from 13 to 54 nM for Osimertinib. Osimertinib (AZD-9291) also potently inhibits phosphorylation of EGFR in T790M mutant cell lines (H1975 (L858R/T790M), PC-9VanR (ex19del/T790M), with mean IC50 potency less than 15 nM[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:PC-9, H3255, PC-9ER, and H1975 cells
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Concentration:0.0001, 0.001, 0.01, 0.1, 1, 10 μM
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Incubation Time:72 hours
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Result:Dramatically inhibited cell proliferation (IC50=41,26, 41, 31 nM, respectively)
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Cell Line:Ba/F3 cells (harboring a T790M mutation, exon 19del+T790M, or L858R+T790M)
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Concentration:0.0001, 0.001, 0.01, 0.1, 1, 10 μM
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Incubation Time:72 hours
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Result:Inhibited cell proliferation (IC50 = 6, 7, 74 nM, respectively)
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Cell Line:Ba/F3 cells (harboring EGFR exon 20 insertion mutations)
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Concentration:0.0001, 0.001, 0.01, 0.1, 1, 10 μM
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Incubation Time:72 hours
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Result:Inhibited cell proliferation (IC50 = 16, 701, 230, 38 nM, respectively)
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Cell Line:Ba/F3 cells(harboring EGFR exon 19del+T790M or EGFR L858R+T790M) [2]
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Concentration:0.1 μM
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Incubation Time:48 hours
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Result:Inducted apoptosis with the rate of 40.9% and 90% in EGFR T790M positive mutations cells respectively.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:PC-9 (ex19del) and H1975 (L858R/T790M) tumor xenograft models[1]
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Dosage:0.1-10 mg/kg (PC-9 xenograft models); 0.5- 25 mg/kg (H1975 xenograft models)
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Administration:p.o.; daily for 14 day
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Result:Induced significant dose-dependent regression in both PC-9 (ex19del) and H1975 (L858R/T790M) tumor xenograft models.
Chemical Information
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CAS No. 1421373-66-1
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Appearance Solid
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Molecular Weight 595.71
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Formula C29H37N7O5S
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Color White to yellow
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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
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Synonyms
AZD-9291 mesylate; Mereletinib mesylate
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
4°C, sealed storage, away from moisture
* In solvent : -80°C, 2 years; -20°C, 1 year (sealed storage, away from moisture)
Publications (194)
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Journal Impact Factor
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Most Recent
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Signal Transduct Target Ther
MUCIN 1 confers inflammatory memory of tyrosine kinase inhibitor resistance in non-small cell lung cancer. [Abstract]2025 Nov 28;10(1):389. PMID: 41309558 -
Science
2026 Mar 26;391(6792):eadz9353. PMID: 41538410 -
Cancer Cell
A pan-KRAS inhibitor and its derived degrader elicit multifaceted anti-tumor efficacy in KRAS-driven cancers. [Abstract]2025 Jul 25:S1535-6108(25)00310-1. PMID: 40780213 -
Cancer Cell
Treatment-Induced Tumor Dormancy through YAP-Mediated Transcriptional Reprogramming of the Apoptotic Pathway. [Abstract]2020 Jan 13;37(1):104-122.e12. PMID: 31935369 -
Eur Heart J
2025 Dec 3:ehaf813. PMID: 41330421 -
Cancer Discov
2019 Jul;9(7):926-943. PMID: 31092401 -
Nat Cancer
Scribble mis-localization induces adaptive resistance to KRAS G12C inhibitors through feedback activation of MAPK signaling mediated by YAP-induced MRAS. [Abstract]2023 Jun;4(6):829-843. PMID: 37277529
Osimertinib mesylate purchased from MedChemExpress. Usage Cited in: Nat Cancer. 2023 Jun;4(6):829-843. [Abstract]
HCC827 (EGFR mutant) and NCI-H2228 (ALK-translocated) lung cancer cells were treated with 100 nM of the EGFR inhibitor Osimertinib or 500 nM of the ALK inhibitor alectinib for 72 h, respectively. Representative immunofluorescence images of E-cadherin were merged with DAPI. Scale bar, 10 μm.
Osimertinib mesylate purchased from MedChemExpress. Usage Cited in: Nat Cancer. 2023 Jun;4(6):829-843. [Abstract]
HCC827 and NCI-H2228 cancer cell lines were treated with 100 nM Osimertinib, 500 nM alectinib or 50 nM trametinib for 72 h as indicated. Immunofluorescence images of Scrib were merged with DAPI. Scale bar, 10 μm.
Osimertinib mesylate purchased from MedChemExpress. Usage Cited in: Nat Cancer. 2023 Jun;4(6):829-843. [Abstract]
Osimertinib-induced MRAS activation was abrogated by the addition of either SHP2 or SOS1 inhibitor in HCC827 cells. HCC827 cells were treated with 100 nM Osimertinib with or without 10 μM BI-3406 or 10 μM SHP099 for 72 h.
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Nat Cancer
An allosteric inhibitor against the therapy-resistant mutant forms of EGFR in non-small cell lung cancer. [Abstract]2022 Apr;3(4):402-417. PMID: 35422503 -
Adv Mater
Highly Specific Cytokine Receptor-Targeting Chimeras for Targeted Membrane Protein Degradation and Sensitization of Osimertinib in EGFR-Mutated Non-Small-Cell Lung Cancer. [Abstract]2025 May 22:e2504050. PMID: 40401615 -
Drug Resist Updat
Stabilin-1+ lipid-associated macrophages promote lung adenocarcinoma liver metastasis and osimertinib resistance through impairing macrophage phagocytosis via SIRPα-CD47 axis. [Abstract]2026 May:86:101379. PMID: 41719890 -
Cancer Res
Enozertinib is a Selective, Brain-penetrant EGFR inhibitor for Treating Non-small Cell Lung Cancers with EGFR Exon 20 and Atypical Mutations. [Abstract]2025 Nov 6. PMID: 41196054 -
Mol Cell
Amplified dosage of the NKX2-1 lineage transcription factor controls its oncogenic role in lung adenocarcinoma. [Abstract]2025 Mar 21:S1097-2765(25)00194-7. PMID: 40139189 -
Cancer Res
Loss of CDKN2A Enhances the Efficacy of Immunotherapy in EGFR-Mutant Non-Small Cell Lung Cancer. [Abstract]2025 Feb 1;85(3):585-601. PMID: 39514336 -
Cancer Res
Osimertinib covalently binds to CD34 and eliminates myeloid leukemia stem/progenitor cells. [Abstract]2024 Feb 1;84(3):479-492. PMID: 38095536 -
Cancer Res
RBM10 Loss Promotes EGFR-Driven Lung Cancer and Confers Sensitivity to Spliceosome Inhibition. [Abstract]2023 May 2;83(9):1490-1502. PMID: 36853175 -
Cancer Res
Metabolic reprogramming driven by IGF2BP3 promotes acquired resistance to EGFR inhibitors in non-small cell lung cancer. [Abstract]2023 Jul 5;83(13):2187-2207. PMID: 37061993 -
ACS Nano
An Osimertinib-Perfluorocarbon Nanoemulsion with Excellent Targeted Therapeutic Efficacy in Non-small Cell Lung Cancer: Achieving Intratracheal and Intravenous Administration. [Abstract]2022 Aug 23;16(8):12590-12605. PMID: 35863049 -
Nat Commun
B7-H3-mediated cis-inhibition of EGFR by a tumor-selective bispecific antibody enhances anti-tumor efficacy and minimizes toxicities. [Abstract]2026 Feb 24;17(1):3113. PMID: 41735305 -
Nat Commun
An alternative EGFR activation by patient-derived R252C mutation promotes cancer progression. [Abstract]2026 Jan 21;17(1):1902. PMID: 41565660 -
Cell Death Differ
PD-L2 drives resistance to EGFR-TKIs: dynamic changes of the tumor immune environment and targeted therapy. [Abstract]2024 Sep;31(9):1140-1156. PMID: 38816578 -
Adv Sci (Weinh)
CauFinder: Steering Cell-State and Phenotype Transitions by Causal Disentanglement Learning. [Abstract]2026 Jun 16:e76177. PMID: 42301228 -
Adv Sci (Weinh)
Splicing Shift of RAC1 Accelerates Tumorigenesis and Defines a Potent Therapeutic Target in Lung Cancer. [Abstract]2025 Jun 23:e03322. PMID: 40548642 -
Adv Sci (Weinh)
Addressing Clinical Limitations of Glutaminase Inhibitors: Novel Strategies for Osimertinib-Resistant Lung Cancer by Exploiting Glutamine Metabolic Dependency. [Abstract]2024 Dec 16:e2411479. PMID: 39680480 -
Adv Sci (Weinh)
Brain Metastasis from EGFR-Mutated Non-Small Cell Lung Cancer: Secretion of IL11 from Astrocytes Up-Regulates PDL1 and Promotes Immune Escape. [Abstract]2024 Jul;11(26):e2306348. PMID: 38696655 -
Exp Hematol Oncol
Combined inhibition of MET and VEGF enhances therapeutic efficacy of EGFR TKIs in EGFR-mutant non-small cell lung cancer with concomitant aberrant MET activation. [Abstract]2024 Oct 1;13(1):97. PMID: 39354638 -
Theranostics
Endogenous glutamate determines ferroptosis sensitivity via ADCY10-dependent YAP suppression in lung adenocarcinoma. [Abstract]2021 Mar 24;11(12):5650-5674. PMID: 33897873 -
Theranostics
ILT4 inhibition prevents TAM- and dysfunctional T cell-mediated immunosuppression and enhances the efficacy of anti-PD-L1 therapy in NSCLC with EGFR activation. [Abstract]2021 Jan 19;11(7):3392-3416. PMID: 33537094 -
J Exp Clin Cancer Res
Hypoxia-inducible APCDD1L-AS1 promotes osimertinib resistance by stabilising DLST to drive tricarboxylic acid cycle in lung adenocarcinoma. [Abstract]2025 Jul 9;44(1):197. PMID: 40634956 -
J Exp Clin Cancer Res
RBM10 deficiency promotes brain metastasis by modulating sphingolipid metabolism in a BBB model of EGFR mutant lung adenocarcinoma. [Abstract]2025 Mar 11;44(1):95. PMID: 40069781 -
J Exp Clin Cancer Res
The third-generation EGFR inhibitor AZD9291 overcomes primary resistance by continuously blocking ERK signaling in glioblastoma. [Abstract]2019 May 23;38(1):219. PMID: 31122294
Osimertinib mesylate purchased from MedChemExpress. Usage Cited in: J Exp Clin Cancer Res. 2019 May 23;38(1):219. [Abstract]
Measurement of antiproliferation effects of AZD9291 (Osimertinib) (0.5-2 μM; 24 h) by EdU incorporation assay.
Osimertinib mesylate purchased from MedChemExpress. Usage Cited in: J Exp Clin Cancer Res. 2019 May 23;38(1):219. [Abstract]
U87 and U251 cells are exposed to indicated concentrations of AZD9291 (Osimertinib) for 24 h and then stimulated with EGF (100 ng/mL) for 30 min. Cell lysates are prepared and examined using Western blot analysis with indicated antibodies.
Osimertinib mesylate purchased from MedChemExpress. Usage Cited in: J Exp Clin Cancer Res. 2019 May 23;38(1):219. [Abstract]
U87 and U251 cells are treated with AZD9291 (Osimertinib) or CP-358774 for 4, 24 and 48 h. The expression level of p-ERK are assessed using Western blot analysis.
Osimertinib mesylate purchased from MedChemExpress. Usage Cited in: J Exp Clin Cancer Res. 2019 May 23;38(1):219. [Abstract]
GBM cells were treated by different concentrations of AZD9291 (Osimertinib) (0.625–20 μM) for 72 h. The cell viability was examined by CCK8 assay. Comparation of different sensitive of GBM cells to EGFR inhibitors (AZD9291, Erlotinib and Gefitinib).
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J Exp Clin Cancer Res
Co-administration of 20(S)-protopanaxatriol (g-PPT) and EGFR-TKI overcomes EGFR-TKI resistance by decreasing SCD1 induced lipid accumulation in non-small cell lung cancer. [Abstract]2019 Mar 15;38(1):129. PMID: 30876460 -
Sci Adv
A genome-wide genetic screen reveals the P2Y2-integrin axis as a stabilizer of EGFR mutants in non-small cell lung cancer (NSCLC). [Abstract]2026 Jan 23;12(4):eadv3980. PMID: 41564171 -
Sci Adv
Targeting RRM2 with dual-modal theranostic smart nanoresponder overcomes osimertinib resistance and triggers immune remodeling in NSCLC. [Abstract]2025 Oct 17;11(42):eady7930. PMID: 41105786 -
Redox Biol
C-terminal interleukin 1 alpha (IL-1α) overexpression drives EMT and a vulnerability to ferroptosis in HNSCC. [Abstract]2026 Jun:93:104172. PMID: 42013543 -
J Control Release
Macropinocytosis-targeted peptide-docetaxel conjugate for bystander pancreatic cancer treatment. [Abstract]2024 Dec:376:829-841. PMID: 39491626 -
Cell Rep Med
Targeting of vulnerabilities of drug-tolerant persisters identified through functional genetics delays tumor relapse. [Abstract]2024 Mar 19;5(3):101471. PMID: 38508142 -
Cell Rep Med
Using patient-derived organoids to predict locally advanced or metastatic lung cancer tumor response: A real-world study. [Abstract]2023 Feb 21;4(2):100911. PMID: 36657446 -
Clin Cancer Res
STX-721, a Covalent EGFR/HER2 Exon 20 Inhibitor, Utilizes Exon 20-Mutant Dynamic Protein States and Achieves Unique Mutant Selectivity Across Human Cancer Models. [Abstract]2025 Jun 4:OF1-OF17. PMID: 40465424 -
Cancer Lett
2025 Apr 10:217715. PMID: 40220852 -
Cancer Lett
A novel EGFR inhibitor acts as potent tool for hypoxia-activated prodrug systems and exerts strong synergistic activity with VEGFR inhibition in vitro and in vivo. [Abstract]2023 Jul 1:565:216237. PMID: 37211067 -
Int J Biol Sci
MUC3A induces PD-L1 and reduces tyrosine kinase inhibitors effects in EGFR-mutant non-small cell lung cancer. [Abstract]2021 Apr 12;17(7):1671-1681. PMID: 33994852 -
Cell Death Dis
Cancer-associated fibroblasts promote osimertinib resistance in non-small cell lung cancer cells via METTL1-mediated NET1 m7G modification. [Abstract]2026 Feb 21;17(1):248. PMID: 41723107 -
Cell Death Dis
Integrative multi-omics identifies AP-1 transcription factor as a targetable mediator of acquired osimertinib resistance in non-small cell lung cancer. [Abstract]2025 May 25;16(1):414. PMID: 40414926 -
Cell Death Dis
MCT1 relieves osimertinib-induced CRC suppression by promoting autophagy through the LKB1/AMPK signaling. [Abstract]2019 Aug 13;10(8):615. PMID: 31409796 -
Cell Death Dis
AXL degradation in combination with EGFR-TKI can delay and overcome acquired resistance in human non-small cell lung cancer cells. [Abstract]2019 May 1;10(5):361. PMID: 31043587 -
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J Pharm Anal
Synergistic effects of methyl 2-cyano-3,11-dioxo-18beta-olean-1,-12-dien-30-oate and erlotinib on erlotinib-resistant non-small cell lung cancer cells. [Abstract]2021 Dec;11(6):799-807. PMID: 35028186 -
Dev Cell
Stress-induced pro-inflammatory glioblastoma stem cells secrete TNFAIP6 to enhance tumor growth and induce suppressive macrophages. [Abstract]2025 May 15:S1534-5807(25)00287-4. PMID: 40403724 -
Int J Biol Macromol
Exploring the association of POSTN+ cancer-associated fibroblasts with triple-negative breast cancer. [Abstract]2024 May;268(Pt 1):131560. PMID: 38631570 -
Acta Pharmacol Sin
Ivacaftor, a CFTR potentiator, synergizes with osimertinib against acquired resistance to osimertinib in NSCLC by regulating CFTR-PTEN-AKT axis. [Abstract]2025 Apr;46(4):1045-1057. PMID: 39627385 -
Acta Pharmacol Sin
Targeting DNA-PK overcomes acquired resistance to third-generation EGFR-TKI osimertinib in non-small-cell lung cancer. [Abstract]2021 Apr;42(4):648-654. PMID: 33414509 -
Acta Pharmacol Sin
Osimertinib successfully combats EGFR-negative glioblastoma cells by inhibiting the MAPK pathway. [Abstract]2021 Jan;42(1):108-114. PMID: 32398685 -
Acta Pharmacol Sin
2019 Dec;40(12):1587-1595. PMID: 31171828
Osimertinib mesylate purchased from MedChemExpress. Usage Cited in: Acta Pharmacol Sin. 2019 Dec;40(12):1587-1595. [Abstract]
MDAMB-453 cells are pre-treated with 10 μM MG132 for 1 h before treatment with the 20 μM AZD for 4 h. Cell lysates were used for SDS PAGE and Western blotting. AZD9291 disrupts the EZH2–EED interaction by binding to EZH2 directly
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Phytomedicine
Halofuginone targets Serine/Glycine synthesis to reverse epidermal growth factor receptor Tyrosine Kinase inhibitor resistance in lung adenocarcinoma. [Abstract]2025 Jul 25:143:156788. PMID: 40354707 -
Free Radic Biol Med
Targeting PDK4 to mitigate osimertinib-induced cardiotoxicity: Insights into mitochondria-endoplasmic reticulum crosstalk and necroptosis. [Abstract]2025 Aug 9:240:267-283. PMID: 40789497 -
NPJ Precis Oncol
High-throughput screening identifies NT-1 that synergizes with MRTX1133 against acquired resistant KRASG12D colorectal cancer. [Abstract]2026 Apr 8;10(1):211. PMID: 41951768 -
NPJ Precis Oncol
GLMP promotes EGFR-TKI resistance by activating autophagy and RhoA pathway in non-small cell lung cancer. [Abstract]2025 Nov 26;9(1):391. PMID: 41298761 -
Neoplasia
The antitumor activity of osimertinib plus palbociclib in non-small cell lung cancer patient-derived xenograft (PDX)/2D/3D culture models harboring EGFR amplification and CDKN2A/2B homozygous deletions. [Abstract]2024 Aug 14:57:101039. PMID: 39146623 -
Biomed Pharmacother
2024 Feb:171:116124. PMID: 38198957 -
Oncogene
Amphiregulin drives EGFR-dependent genome stability in colorectal cancer and represents a targetable vulnerability. [Abstract]2026 Jun 15. PMID: 42298179 -
Oncogene
2025 Dec 16. PMID: 41402633 -
Stem Cell Res Ther
L-Glutamate enables the EGFR-MEK-ERK-mTFB2 axis to enhance mitochondrial biogenesis in intestinal stem cells. [Abstract]2025 Oct 31;16(1):599. PMID: 41174788 -
Oncogene
Cancer-associated fibroblasts promote EGFR-TKI resistance via the CTHRC1/glycolysis/H3K18la positive feedback loop. [Abstract]2025 May;44(19):1400-1414. PMID: 40011576 -
Oncogene
NEU4-mediated desialylation enhances the activation of the oncogenic receptors for the dissemination of ovarian carcinoma. [Abstract]2024 Nov;43(49):3556-3569. PMID: 39402373 -
Oncogene
PrPC controls epithelial-to-mesenchymal transition in EGFR-mutated NSCLC: implications for TKI resistance and patient follow-up. [Abstract]2024 Sep;43(37):2781-2794. PMID: 39147880 -
Oncogene
CRL2KLHDC3 mediates p14ARF N-terminal ubiquitylation degradation to promote non-small cell lung carcinoma progression. [Abstract]2022 May;41(22):3104-3117. PMID: 35468939 -
Cell Chem Biol
2026 Feb 11:S2451-9456(26)00027-9. PMID: 41679298 -
J Natl Cancer Inst
Suppressing c-FOS expression by G-quadruplex ligands inhibits osimertinib-resistant non-small cell lung cancers. [Abstract]2023 Nov 8;115(11):1383-1391. PMID: 37481710 -
Cell Chem Biol
Overcoming Resistance to Targeted Anticancer Therapies through Small-Molecule-Mediated MEK Degradation. [Abstract]2018 Aug 16;25(8):996-1005.e4. PMID: 29909991
Osimertinib mesylate purchased from MedChemExpress. Usage Cited in: Cell Chem Biol. 2018 Aug 16;25(8):996-1005.e4. [Abstract]
Negligible increases in caspase-3 activity or PARP-1 cleavage is observed in H1975 NSCLC cells treated with DMSO, single agent PAC-1 (5 mM), or Osimertinib (Osi). In cells treated with PAC-1+Osimertinib, dramatic increases in caspase-3 activity is observed as early as 36 hr post treatment.
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Cell Rep
circATF6 triggers calcium overload to synergize with EGFR-TKI in non-small cell lung cancer via modulation of proteostasis. [Abstract]2025 Dec 5;44(12):116659. PMID: 41351835 -
Cell Rep
A MYC-STAMBPL1-TOE1 positive feedback loop mediates EGFR stability in hepatocellular carcinoma. [Abstract]2024 Oct 8;43(10):114812. PMID: 39388352 -
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J Med Chem
Don't Lose Your (War)head: Structure-Activity Relationships of Covalent Warheads as Substrates for GST-Catalyzed Glutathione Conjugation. [Abstract]2026 May 14;69(9):11574-11591. PMID: 42062179 -
J Med Chem
2025 Aug 28;68(16):17917-17932. PMID: 40801664 -
J Med Chem
Bioactivity-Driven Synthesis of the Marine Natural Product Naamidine J and Its Derivatives as Potential Tumor Immunological Agents by Inhibiting Programmed Death-Ligand 1. [Abstract]2023 Apr 27;66(8):5427-5438. PMID: 37040446 -
J Med Chem
Discovery of (R)-1-(3-(4-Amino-3-(3-chloro-4-(pyridin-2-ylmethoxy)phenyl)-1H-pyrazolo[3,4-d]pyrimidin-1-yl)piperidin-1-yl)prop-2-en-1-one (CHMFL-EGFR-202) as a Novel Irreversible EGFR Mutant Kinase Inhibitor with a Distinct Binding Mode. [Abstract]2017 Apr 13;60(7):2944-2962. PMID: 28282122 -
Int J Nanomedicine
A Hybrid Protein-Oxygen Nanomedicine Overcomes Osimertinib Resistance in NSCLC via HIF-1α/VEGF/EGFR Inhibition. [Abstract]2025 Aug 27:20:10389-10405. PMID: 40901248 -
Ecotoxicol Environ Saf
PPARγ-responsive luciferase reporter system for high-throughput screening of chemical toxins with potential pulmonary fibrosis effects. [Abstract]2025 Nov 15:307:119433. PMID: 41273832 -
Cancer Cell Int
SHP2 inhibition enhances the anticancer effect of Osimertinib in EGFR T790M mutant lung adenocarcinoma by blocking CXCL8 loop mediated stemness. [Abstract]2021 Jul 3;21(1):337. PMID: 34217295 -
Cancer Cell Int
Trichostatin A downregulates bromodomain and extra-terminal proteins to suppress osimertinib resistant non-small cell lung carcinoma. [Abstract]2021 Apr 15;21(1):216. PMID: 33858423 -
Int J Mol Med
Suppression of tumor growth by GMI, an edible fungal immunomodulatory protein, is associated with targeting GSK3β‑mediated proteasomal degradation of PD‑L1. [Abstract]2025 Dec;56(6):217. PMID: 41070618 -
Int J Mol Med
Characterization of circRNAs in established osimertinib‑resistant non‑small cell lung cancer cell lines. [Abstract]2023 Nov;52(5):102. PMID: 37681495 -
Heart Rhythm
Osimertinib induces prolongation of action potential duration via downregulation of KCNN1 expression: Exploring the potential mechanisms of arrhythmia. [Abstract]2025 Jul 11:S1547-5271(25)02640-2. PMID: 40653133 -
Biochem Pharmacol
Lysine methylation-mediated SMYD2 degradation by casticin sensitizes non-small-cell lung cancer cells to osimertinib therapy. [Abstract]2026 Jan;243(Pt 2):117562. PMID: 41314435 -
Biochem Pharmacol
Targeting N6-methyladenosine demethylase FTO overcomes osimertinib resistance by inducing G0/G1 phase arrest in an m6A-dependent manner in lung adenocarcinoma. [Abstract]2025 Jul 29;242(Pt 1):117198. PMID: 40744230 -
Pharmaceutics
Inhalable Anti-EGFR Antibody-Conjugated Osimertinib Liposomes for Non-Small Cell Lung Cancer. [Abstract]2024 Nov 12;16(11):1444. PMID: 39598567 -
Mol Cancer Ther
AMT-562, a Novel HER3-targeting Antibody-Drug Conjugate, Demonstrates a Potential to Broaden Therapeutic Opportunities for HER3-expressing Tumors. [Abstract]2023 Sep 5;22(9):1013-1027. PMID: 37302522 -
Drug Deliv Transl Res
Pulmonary delivery of osimertinib liposomes for non-small cell lung cancer treatment: formulation development and in vitro evaluation. [Abstract]2022 Oct;12(10):2474-2487. PMID: 34816394 -
Mol Cancer Ther
TAS-121, A Selective Mutant EGFR Inhibitor, Shows Activity Against Tumors Expressing Various EGFR Mutations Including T790M and Uncommon Mutations G719X. [Abstract]2019 May;18(5):920-928. PMID: 30872380 -
Mol Cancer Ther
Afatinib Is a New Therapeutic Approach in Chordoma with a Unique Ability to Target EGFR and Brachyury. [Abstract]2018 Mar;17(3):603-613. PMID: 29237806 -
J Ethnopharmacol
Taxus chinensis var. mairei (Lemée et Lévl) Cheng et L.K. Fu overcomes the resistance to osimertinib in EGFR-mutant non-small-cell lung cancer via suppression of ERK1/2-related cholesterol biosynthesis. [Abstract]2024 Jul 18:118586. PMID: 39032664 -
Int J Pharm
Microfluidic-assisted preparation of ARV 825 and Osimertinib loaded liposomal formulation as a potential system for colorectal cancer therapy. [Abstract]2025 Dec 25:686:126358. PMID: 41192598 -
Cancer Drug Resist
Novel FAK inhibitors suppress tumor growth and reverse EGFR-TKI resistance in non-small cell lung cancer. [Abstract]2025 Nov 5:8:57. PMID: 41281943 -
Commun Biol
2025 Nov 29. PMID: 41318855 -
Commun Biol
EGFR signaling and pharmacology in oncology revealed with innovative BRET-based biosensors. [Abstract]2024 Mar 1;7(1):250. PMID: 38429428 -
Commun Biol
A small-molecule compound D6 overcomes EGFR-T790M-mediated resistance in non-small cell lung cancer. [Abstract]2021 Dec 13;4(1):1391. PMID: 34903832 -
Respir Res
Combination of betulinic acid and EGFR-TKIs exerts synergistic anti-tumor effects against wild-type EGFR NSCLC by inducing autophagy-related cell death via EGFR signaling pathway. [Abstract]2024 May 20;25(1):215. PMID: 38764025 -
Cancer Gene Ther
YAP 5-methylcytosine modification increases its mRNA stability and promotes the transcription of exosome secretion-related genes in lung adenocarcinoma. [Abstract]2023 Jan;30(1):149-162. PMID: 36123390 -
Int J Mol Sci
JAC4 Inhibits EGFR-Driven Lung Adenocarcinoma Growth and Metastasis through CTBP1-Mediated JWA/AMPK/NEDD4L/EGFR Axis. [Abstract]2023 May 15;24(10):8794. PMID: 37240137 -
Int J Oncol
Clinical importance of long non‑coding RNA LINC00460 expression in EGFR‑mutant lung adenocarcinoma. [Abstract]2020 Jan;56(1):243-257. PMID: 31789388 -
Cell Oncol (Dordr)
Proteasomal deubiquitylase activity enhances cell surface recycling of the epidermal growth factor receptor in non-small cell lung cancer. [Abstract]2022 Oct;45(5):951-965. PMID: 36129611 -
Int Immunopharmacol
HMOX1 expression influence the role of macrophage in EGFR-TKI resistance of lung adenocarcinoma. [Abstract]2026 Jan 1;168(Pt 1):115795. PMID: 41205382 -
Bioorg Chem
A pomalidomide-based gefitinib PROTAC degrader effectively inhibits lung cancer progression in EGFR-TKIs-acquired resistant models by targeting EGFR degradation and ETFA-mediated ATP generation. [Abstract]2025 Aug 9:164:108864. PMID: 40815992 -
Mol Cancer Res
METTL14-mediated Bim mRNA m6A modification augments osimertinib sensitivity in EGFR-mutant NSCLC cells. [Abstract]2024 Nov 1;22(11):1051-1063. PMID: 38953880 -
Int Immunopharmacol
Identifying the critical oncogenic mechanism of LDHA based on a prognostic model of T-cell synthetic drivers. [Abstract]2024 Jan 5:126:111265. PMID: 38000233 -
Bioorg Chem
Exploration of novel dihydroquinoxalinone derivatives as EGFRL858R/T790M tyrosine kinase inhibitors for the treatment of non-small-cell lung cancer. [Abstract]2023 Jun:135:106494. PMID: 37011522 -
Eur J Pharmacol
XHL11, a novel selective EGFR inhibitor, overcomes EGFRT790M-mediated resistance in non-small cell lung cancer. [Abstract]2021 Sep 15:907:174297. PMID: 34217707 -
Mol Cancer Res
TAS6417/CLN-081 Is a Pan-Mutation-Selective EGFR Tyrosine Kinase Inhibitor with a Broad Spectrum of Preclinical Activity against Clinically Relevant EGFR Mutations. [Abstract]2019 Nov;17(11):2233-2243. PMID: 31467113 -
Mol Cancer Res
Activation of AXL as a Preclinical Acquired Resistance Mechanism Against Osimertinib Treatment in EGFR-Mutant Non-Small Cell Lung Cancer Cells. [Abstract]2019 Feb;17(2):499-507. PMID: 30463991 -
Cell Rep Methods
Tumor immune microenvironment reconstitution in patient-derived organoids enables therapy modeling for NSCLC. [Abstract]2026 Jun 15;6(6):101339. PMID: 42134319 -
Mol Oncol
Nicotinamide N-methyltransferase promotes drug resistance in lung cancer, as revealed by nascent proteomic profiling. [Abstract]2025 Jul 18. PMID: 40679940 -
Mol Oncol
Inhibition of CDCP1 by 8-isopentenylnaringenin synergizes with EGFR inhibitors in lung cancer treatment. [Abstract]2023 Aug;17(8):1648-1665. PMID: 37013960 -
Cancers
Spironolactone, a Classic Potassium-Sparing Diuretic, Reduces Survivin Expression and Chemosensitizes Cancer Cells to Non-DNA-Damaging Anticancer Drugs. [Abstract]2019 Oct 14;11(10):1550. PMID: 31614999 -
Cancers
Brexpiprazole, a Serotonin-Dopamine Activity Modulator, Can Sensitize Glioma Stem Cells to Osimertinib, a Third-Generation EGFR-TKI, via Survivin Reduction. [Abstract]2019 Jul 5;11(7):947. PMID: 31284441 -
iScience
USP5-mediated CD73 deubiquitination drives osimertinib resistance via PI3K/AKT and glycolysis activation in LUAD. [Abstract]2026 Feb 5;29(3):114916. PMID: 41767275 -
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J Cell Physiol
Overexpression of N-acetylglucosaminyltransferase V promotes human parotid gland acinar cell immortalization via the epidermal receptor activation. [Abstract]2022 Mar;237(3):1780-1789. PMID: 34806177 -
Sci Rep
2026 Mar 20;16(1):14300. PMID: 41862552 -
J Biol Chem
Diarylheptanoid 35d overcomes EGFR TKI resistance by inducing hsp70-mediated lysosomal degradation of EGFR in EGFR-mutant lung adenocarcinoma. [Abstract]2023 Jun;299(6):104814. PMID: 37178919 -
Cancer Res Treat
MLL4 Regulates the Progression of Non-Small-Cell Lung Cancer by Regulating the PI3K/AKT/SOX2 Axis. [Abstract]2023 Jul;55(3):778-803. PMID: 36701842 -
Bioengineering (Basel)
Precision Oncology for High-Grade Gliomas: A Tumor Organoid Model for Adjuvant Treatment Selection. [Abstract]2025 Oct 19;12(10):1121. PMID: 41155119 -
Transl Lung Cancer Res
Development of a 3D-3 co-culture microbead consisting of cancer-associated fibroblasts and human umbilical vein endothelial cells for the anti-tumor drug assessment of lung cancer. [Abstract]2025 Jun 30;14(6):2159-2179. PMID: 40673102 -
Transl Lung Cancer Res
Construction of a lung cancer 3D culture model based on alginate/gelatin micro-beads for drug evaluation. [Abstract]2024 Oct 31;13(10):2698-2712. PMID: 39507032 -
Mol Med Rep
Inhibition of Bcl-2 and Bcl-xL overcomes the resistance to the third-generation EGFR tyrosine kinase inhibitor osimertinib in non-small cell lung cancer. [Abstract]2021 Jan;23(1):48. PMID: 33200796 -
BMC Cancer
METTL16-dependent miR-146b-5p m6A modification remodeling sensitize NSCLC to osimertinib via activating PI3K/AKT signaling. [Abstract]2025 Apr 8;25(1):641. PMID: 40200229 -
Toxicol Appl Pharmacol
Jaceosidin overcomes osimertinib resistance in lung cancer by inducing G2/M cycle arrest through targeting DDB1. [Abstract]2025 Apr 3:117327. PMID: 40187661 -
Cancer Res Commun
Constitutive EGFR Activation Induced by PTPRR Downregulation Confers Resistance to KRAS Inhibitors. [Abstract]2026 Mar 10. PMID: 41808249 -
Basic Clin Pharmacol Toxicol
GMI, a Fungal Immunomodulatory Protein From Ganoderma microsporum, Induces Different Cytotoxicity in Parental and Osimertinib-Resistant EGFR-Mutated Lung Cancer Cells via Apoptotic and Autophagic Cell Death. [Abstract]2025 Dec;137(6):e70143. PMID: 41269207 -
Environ Toxicol
Epithelial growth factor receptor tyrosine kinase inhibitors alleviate house dust mite allergen Der p2-induced IL-6 and IL-8. [Abstract]2019 Apr;34(4):476-485. PMID: 30623574
Osimertinib mesylate purchased from MedChemExpress. Usage Cited in: Environ Toxicol. 2019 Apr;34(4):476-485. [Abstract]
Protein levels of p-EGFR(Tyr1068), p-EGFR(Tyr1137), EGFR, p-STAT3, STAT3, p-AKT, AKT, p-p38 MAPK, and p-ERK MAPK are analyzed in GST-Der pII1-129-stimulated human epithelial cells with/without AZD-9291 treatment.
Osimertinib mesylate purchased from MedChemExpress. Usage Cited in: Environ Toxicol. 2019 Apr;34(4):476-485. [Abstract]
Protein levels of p-EGFR(Tyr1068), p-EGFR(Tyr1137), EGFR, p-STAT3, STAT3, p-AKT, AKT, p-p38 MAPK, and p-ERK MAPK are analyzed in GST-Der pII1-129-stimulated human epithelial cells with/without AZD-9291 treatment.
Osimertinib mesylate purchased from MedChemExpress. Usage Cited in: Environ Toxicol. 2019 Apr;34(4):476-485. [Abstract]
Protein levels of NF-κB and IκB are analyzed are analyzed in GST-Der pII1-129-stimulated human epithelial cells with/without AZD-9291 treatment.
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Front Biosci (Landmark Ed)
Integrated Analysis of Single-cell and Bulk-RNA Sequencing Data to Identify Redox-related Genes as Prognostic Biomarkers and Therapeutic Targets of Lung Adenocarcinoma With Osimertinib Resistance. [Abstract]2025 Sep 25;30(9):40454. PMID: 41074434 -
RSC Chem Biol
A covalent inhibitor of the YAP-TEAD transcriptional complex identified by high-throughput screening. [Abstract]2023 Aug 29;4(11):894-905. PMID: 37920398 -
Mol Pharmacol
Influence of Tyrosine Kinase Inhibition on Organic Anion Transporting Polypeptide 1B3-Mediated Uptake. [Abstract]2022 Jun;101(6):381-389. PMID: 35383108 -
Discov Oncol
Integrative bulk RNA analysis unveils immune evasion mechanisms and predictive biomarkers of osimertinib resistance in non-small cell lung cancer. [Abstract]2025 Aug 12;16(1):1541. PMID: 40796706 -
Am J Cancer Res
Luteolin overcomes acquired resistance to osimertinib in non-small cell lung cancer cells by targeting the HGF-MET-Akt pathway. [Abstract]2023 Sep 15;13(9):4145-4162. PMID: 37818074 -
Genes (Basel)
The Impact of Bevacizumab and miR200c on EMT and EGFR-TKI Resistance in EGFR-Mutant Lung Cancer Organoids. [Abstract]2024 Dec 19;15(12):1624. PMID: 39766891 -
J Chromatogr B Analyt Technol Biomed Life Sci
Simultaneous determination of 11 oral targeted antineoplastic drugs and 2 active metabolites by LC-MS/MS in human plasma and its application to therapeutic drug monitoring in cancer patients. [Abstract]2024 Apr 15:1237:124100. PMID: 38547701 -
PLoS One
A novel small molecule screening assay using normal human chondrocytes toward osteoarthritis drug discovery. [Abstract]2024 Nov 1;19(11):e0308647. PMID: 39485774 -
World J Gastrointest Oncol
Interleukin-22 promotes cancer stemness and chemotherapy resistance in colorectal cancer via epidermal growth factor receptor/extracellular signal-regulated kinase pathway. [Abstract]2025 Aug 15;17(8):108535. PMID: 40837778 -
J Nat Med
Effects of Ephedra Herb extract on the expression of EGFR-activating mutations and c-Met in non-small-cell lung cancer cell line, H1975, and its combined effects with osimertinib. [Abstract]2023 Jun;77(3):523-534. PMID: 37043119 -
Fundam Clin Pharmacol
2021 Oct;35(5):919-929. PMID: 33523504 -
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Eur J Drug Metab Pharmacokinet
Differential Inhibition of Equilibrative Nucleoside Transporter 1 (ENT1) Activity by Tyrosine Kinase Inhibitors. [Abstract]2021 Sep;46(5):625-635. PMID: 34275128 -
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Biochem Biophys Res Commun
Investigating NanoLuc-EGFR engineered cell lines for real-time monitoring of EGFR protein dynamics in live cells. [Abstract]2024 Sep 19:733:150711. PMID: 39312880 -
Oncol Lett
Upregulation of long non‑coding RNA LINC00460 in EGFR‑mutant lung cancer indicates a poor prognosis in patients treated with osimertinib. [Abstract]2023 Jul 20;26(3):380. PMID: 37559586 -
Drug Metab Pharmacokinet
2020 Oct;35(5):456-465. PMID: 32847720 -
Genes Genomics
CKAP4 is a potential therapeutic target to overcome resistance to EGFR-TKIs in lung adenocarcinoma. [Abstract]2025 Mar;47(3):331-340. PMID: 39704929 -
Cytotechnology
Silencing of LINC01278 promotes sensitivity of non-small cell lung cancer cells to osimertinib by targeting miR-324-3p/ZFX axis. [Abstract]2025 Feb;77(1):23. PMID: 39711969 -
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Anticancer Res
Antitumor Potential of Guttiferone E Combined With Carboplatin Against Osimertinib-resistant H1975 Lung Cancer Through Apoptosis. [Abstract]2024 Oct;44(10):4175-4188. PMID: 39348999 -
Int J Anal Chem
An UPLC-MS/MS Method for Determination of Osimertinib in Rat Plasma: Application to Investigating the Effect of Ginsenoside Rg3 on the Pharmacokinetics of Osimertinib. [Abstract]2020 Dec 28:2020:8814214. PMID: 33456471 -
Anticancer Res
Brexpiprazole Reduces Survivin and Reverses EGFR Tyrosine Kinase Inhibitor Resistance in Lung and Pancreatic Cancer. [Abstract]2019 Sep;39(9):4817-4828. PMID: 31519584 -
Am J Transl Res
EGFR/EGFRvIII partly regulates the tumourigenesis of glioblastoma through the SOX9-GLUT3 axis. [Abstract]2021 Jun 15;13(6):6055-6065. PMID: 34306344 -
Respir Physiol Neurobiol
The Cosmc-mediated effects of neutrophil elastase on T antigen expression in BEAS-2B cells. [Abstract]2020 Oct;281:103496. PMID: 32683071 -
Biol Methods Protoc
Optimizing drug sensitivity assays in patient-derived tumor organoids: a comparison of IC50 estimation methods and experimental parameters. [Abstract]2025 Feb 13;10(1):bpaf012. PMID: 40060949 -
Xenobiotica
Changes in gefitinib, erlotinib and osimertinib pharmacokinetics under various gastric pH levels following oral administration of omeprazole and vonoprazan in rats. [Abstract]2018 Nov;48(11):1106-1112. PMID: 29057719 -
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Genome-wide profiling identifies the genetic dependencies of cell death following EGFR inhibition. [Abstract]2025 Apr 9:2025.04.04.647273. PMID: 40291701 -
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Dosage amplification dictates oncogenic regulation by the NKX2-1 lineage factor in lung adenocarcinoma. [Abstract]2023 Oct 27:2023.10.26.563996. PMID: 37994369 -
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Targeting the Golgi apparatus to overcome acquired resistance of non-small cell lung cancer cells to EGFR tyrosine kinase inhibitors. [Abstract]2017 Dec 6;9(2):1641-1655. PMID: 29416720 -
Genes Cancer
NSCLC depend upon YAP expression and nuclear localization after acquiring resistance to EGFR inhibitors. [Abstract]2017 Mar;8(3-4):497-504. PMID: 28680534 -
Oncotarget
Discovery and characterization of a novel irreversible EGFR mutants selective and potent kinase inhibitor CHMFL-EGFR-26 with a distinct binding mode. [Abstract]2017 Mar 14;8(11):18359-18372. PMID: 28407693
Osimertinib mesylate purchased from MedChemExpress. Usage Cited in: Oncotarget. 2017 Mar 14;8(11):18359-18372. [Abstract]
In all of the cell lines tested, AZD9291 (Osimertinib) significantly affects the phosphorylation of eIF4E, which presumably is due to its strong inhibitory activity against MNK2 kinase.
Osimertinib mesylate purchased from MedChemExpress. Usage Cited in: Oncotarget. 2017 Mar 14;8(11):18359-18372. [Abstract]
In all of the cell lines tested, AZD9291 (Osimertinib) significantly affects the phosphorylation of eIF4E, which presumably is due to its strong inhibitory activity against MNK2 kinase.
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Oncotarget
2016 Oct 25;7(43):69760-69769. PMID: 27626175 -
Oncotarget
Ibrutinib selectively and irreversibly targets EGFR (L858R, Del19) mutant but is moderately resistant to EGFR (T790M) mutant NSCLC Cells. [Abstract]2015 Oct 13;6(31):31313-22. PMID: 26375053
Osimertinib mesylate purchased from MedChemExpress. Usage Cited in: Oncotarget. 2015 Oct 13;6(31):31313-22. [Abstract]
Effect of PCI-32765, WZ4002, AZD9291 (Osimertinib) and CO1686 on EGFR phosphorylation of tyrosines 1068 and 1173 in EGFR-dependent cancer cell lines.
Solvent & Solubility
DMSO : 11.67 mg/mL (19.59 mM; ultrasonic and warming and heat to 60°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year (sealed storage, away from moisture). When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year (sealed storage, away from moisture). When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 1.39 mg/mL (2.33 mM); Clear solution
This protocol yields a clear solution of ≥ 1.39 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (13.9 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 1.39 mg/mL (2.33 mM); Clear solution
This protocol yields a clear solution of ≥ 1.39 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (13.9 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL. * In solvent : -80°C, 2 years; -20°C, 1 year (sealed storage, away from moisture)
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation
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Data Sheet (286 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Portuguese - PT (393 KB)
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Handling Instructions (2659 KB)
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. [Content Brief]
[2]. [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. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year (sealed storage, away from moisture). When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 1.6787 mL | 8.3933 mL | 16.7867 mL | 41.9667 mL |
| 5 mM | 0.3357 mL | 1.6787 mL | 3.3573 mL | 8.3933 mL | |
| 10 mM | 0.1679 mL | 0.8393 mL | 1.6787 mL | 4.1967 mL | |
| 15 mM | 0.1119 mL | 0.5596 mL | 1.1191 mL | 2.7978 mL |