Art. -Nr.: HY-15772A

Osimertinib mesylate

Name: Osimertinib mesylate
Brand: MedChemExpress
SKU: HY-15772A
Price: 60.00 USD
Availability: InStock
Rating: 5 (208 reviews)

(Synonyms: AZD-9291 mesylate; Mereletinib mesylate)

208 Cited Publications

Kundenbewertung

Based on 208 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.

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Reinheit : 99.97%
CAS. Nr.: 1421373-66-1
Formel: C₂₉H₃₇N₇O₅S
Molecular Weight:595.71

Speicherung:

4°C, sealed storage, away from moisture

* In solvent : -80°C, 2 years; -20°C, 1 year (sealed storage, away from moisture)

Osimertinib mesylate Chemical Structure

CAS. Nr.: 1421373-66-1

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Use of MCE Products

Antibody-Drug Conjugates

One-stop solution for XDC (ADC/PDC/RDC/ApDC/FDC/ISAC/VDC/SMDC)

Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- In Vitro
- In Vivo
Chemical Information
Publications (208)
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

IC₅₀ & Target

^[1]

EGFR^L858R/T790M

1 nM (IC₅₀)

EGFR^L858R

12 nM (IC₅₀)

Alle EGFR Isoform-spezifische Produkte anzeigen :

In Vitro

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.

Cell Proliferation Assay^[2]

Cell Line:

PC-9, H3255, PC-9ER, and H1975 cells
Concentration:

0.0001, 0.001, 0.01, 0.1, 1, 10 μM
Incubation Time:

72 hours
Result:

Dramatically inhibited cell proliferation (IC₅₀=41,26, 41, 31 nM, respectively)

Cell Proliferation Assay^[2]

Cell Line:

Ba/F3 cells (harboring a T790M mutation, exon 19del+T790M, or L858R+T790M)
Concentration:

0.0001, 0.001, 0.01, 0.1, 1, 10 μM
Incubation Time:

72 hours
Result:

Inhibited cell proliferation (IC₅₀ = 6, 7, 74 nM, respectively)

Cell Proliferation Assay^[2]

Cell Line:

Ba/F3 cells (harboring EGFR exon 20 insertion mutations)
Concentration:

0.0001, 0.001, 0.01, 0.1, 1, 10 μM
Incubation Time:

72 hours
Result:

Inhibited cell proliferation (IC₅₀ = 16, 701, 230, 38 nM, respectively)

Apoptosis Analysis^[2]

Cell Line:

Ba/F3 cells(harboring EGFR exon 19del+T790M or EGFR L858R+T790M) ^[2]
Concentration:

0.1 μM
Incubation Time:

48 hours
Result:

Inducted apoptosis with the rate of 40.9% and 90% in EGFR T790M positive mutations cells respectively.

In Vivo

The tumor-bearing mice are treated with Osimertinib (AZD-9291) (5 mg/kg/day) for one to two weeks. Within days of treatment, 5 of 5 C/L858R mice displays nearly 80% reduction in tumor volume by magnetic resonance imaging MRI after therapy with Osimertinib, while 5 of 5 mice treated with vehicle shows tumor growth^[1]. Osimertinib (AZD-9291) demonstrates improved rat PK, reduced hERG affinity, and improved IGF1R margins relative to the previously described compounds, and so this compound is selected for further investigation. Osimertinib (AZD-9291) also offers an additional degree of broader chemical and profile diversity when compared to the previously described lead compounds. Upon dosing Osimertinib (AZD-9291) in three efficacy models, The comparable efficacy is observed at relatively low doses (10 mg/kg per day). The excellent efficacy is also observed when Osimertinib (AZD-9291) is dosed at 5 mg/kg per day^[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:

PC-9 (ex19del) and H1975 (L858R/T790M) tumor xenograft models^[1]
Dosage:

0.1-10 mg/kg (PC-9 xenograft models); 0.5- 25 mg/kg (H1975 xenograft models)
Administration:

p.o.; daily for 14 day
Result:

Induced significant dose-dependent regression in both PC-9 (ex19del) and H1975 (L858R/T790M) tumor xenograft models.

Chemical Information

CAS. Nr. 1421373-66-1
Appearance Solid
Molecular Weight 595.71
Formel C₂₉H₃₇N₇O₅S
Color White to yellow
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
Synonyms

AZD-9291 mesylate; Mereletinib mesylate
Versand

Room temperature in continental US; may vary elsewhere.
Speicherung

4°C, sealed storage, away from moisture

* In solvent : -80°C, 2 years; -20°C, 1 year (sealed storage, away from moisture)

Publications (208)

All IFBio/Physico-chemical AssayFlow CytometryWBIn Vivo Efficacy StudyCell Proliferation/Viability Assay

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Journal Impact Factor

Signal Transduct Target Ther

Dual-targeting pharmacological UFMylation inhibition reprograms tumor and immune microenvironments to achieve long-term glioblastoma regression. [Abstract]

2026 Jul 20;11(1):281. PMID: 42472853
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
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

Osimertinib mesylate purchased from MedChemExpress. Usage Cited in: Cancer Cell. 2025 Jul 25:S1535-6108(25)00310-1. [Abstract]

Cells were treated for 72 h with the indicated concentrations of compounds (Osimertinib, etc.), and cell viability wasdetermined. Synergy scores (ZIP values) were calculated using the Zero Interaction Potency (ZIP)model in SynergyFinder (n = 3).

Osimertinib mesylate purchased from MedChemExpress. Usage Cited in: Cancer Cell. 2025 Jul 25:S1535-6108(25)00310-1. [Abstract]

Cells were treated for 72 h with the indicated concentrations of compounds (Osimertinib, etc.), and cell viability wasdetermined. Synergy scores (ZIP values) were calculated using the Zero Interaction Potency (ZIP)model in SynergyFinder (n = 3).

Osimertinib mesylate purchased from MedChemExpress. Usage Cited in: Cancer Cell. 2025 Jul 25:S1535-6108(25)00310-1. [Abstract]

Cells were treated for 72 h with the indicated concentrations of compounds (Osimertinib, etc.), and cell viability wasdetermined. Synergy scores (ZIP values) were calculated using the Zero Interaction Potency (ZIP)model in SynergyFinder (n = 3).

Osimertinib mesylate purchased from MedChemExpress. Usage Cited in: Cancer Cell. 2025 Jul 25:S1535-6108(25)00310-1. [Abstract]

Cells were treated for 72 h with the indicated concentrations of compounds (Osimertinib, etc.), and cell viability wasdetermined. Synergy scores (ZIP values) were calculated using the Zero Interaction Potency (ZIP)model in SynergyFinder (n = 3).
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
Science

A genetically encoded device for transcriptome storage in mammalian cells. [Abstract]

2026 Mar 26;391(6792):eadz9353. PMID: 41538410

Osimertinib mesylate purchased from MedChemExpress. Usage Cited in: Science. 2026 Mar 26;391(6792):eadz9353. [Abstract]

Cell viability of PC9 cells treated with the indicated concentrations of Osimertinib (4 days). (n = 3 independent culture replicates). Red arrow represents concentration used for subsequent experiments.

Osimertinib mesylate purchased from MedChemExpress. Usage Cited in: Science. 2026 Mar 26;391(6792):eadz9353. [Abstract]

Representative immunofluorescence images of PC9 cells stained for PI3 (green), FN1 (red), and nuclei [4′,6-diamidino-2-phenylindole (DAPI), blue] with or without 100 nM Osimertinib (4 days) treatment (scale bar, 50 μm).
Eur Heart J

Osimertinib induces reversible cardiac dysfunction through the GATA4-MYLK3-MYL2 axis. [Abstract]

2025 Dec 3:ehaf813. PMID: 41330421

Osimertinib mesylate purchased from MedChemExpress. Usage Cited in: Eur Heart J. 2025 Dec 3:ehaf813. [Abstract]

There was marked sarcomere disarray with evidence of sarcomere fragmentation and aggregation upon 7-day treatment of Osimertinib (0.1-1 μM) in induced pluripotent stem cell-derived cardiomyocytes.

Osimertinib mesylate purchased from MedChemExpress. Usage Cited in: Eur Heart J. 2025 Dec 3:ehaf813. [Abstract]

Osimertinib treatment (0.01–10 µM; 7 days) led to dose-dependent reduction in systolic (area under the curve, peak height, and departure velocity) measures in induced pluripotent stem cell-derived cardiomyocytes. n = 12 per group.

Osimertinib mesylate purchased from MedChemExpress. Usage Cited in: Eur Heart J. 2025 Dec 3:ehaf813. [Abstract]

There was a significant decrease in the protein level of MYLK3 following 7-day treatment of Osimertinib (1 µM). Additionally, MYL2 phosphorylation was also significantly reduced.

Osimertinib mesylate purchased from MedChemExpress. Usage Cited in: Eur Heart J. 2025 Dec 3:ehaf813. [Abstract]

Eight-week-old wild-type mice were subjected to transverse aortic constriction. After 1 week, Osimertinib (Osi, 25 mg/kg; oral gavage; once daily)-only treatment was conducted in Group 1, and Osimertinib and omecamtiv co-treatment was performed in Group 2. After another 2 weeks, omecamtiv treatment was initiated for the Osimertinib-only mice (Group 1). Echocardiography was conducted every week. Omecamtiv co-treatment effectively prevented left ventricular contractile dysfunction by Osimertinib in the course of 2 weeks, as revealed by an increase of ejection fraction and fractional shortening. When Osimertinib-treated mice with apparent cardiac dysfunction were introduced to omecamtiv co-treatment later, there was restoration of left ventricular contractile function.
Cancer Discov

Single and Dual Targeting of Mutant EGFR with an Allosteric Inhibitor. [Abstract]

2019 Jul;9(7):926-943. PMID: 31092401
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 Aug;37(32):e2504050. PMID: 40401615

Osimertinib mesylate purchased from MedChemExpress. Usage Cited in: Adv Mater. 2025 Aug;37(32):e2504050. [Abstract]

The cell viability of Osimertinib -resistant H1975^OE cells pre-treated without (Control) or with 500 nM AP-CRTAC^EGFR for 6 h, followed by 48 h of exposure to various concentrations of Osimertinib (Osi). The results of cell viability assay demonstrated that H1975^OE cells exhibited resistance to Osimertinib, but AP-CRTAC^EGFR increased the sensitivity of H1975OE cells to Osimertinib.

Osimertinib mesylate purchased from MedChemExpress. Usage Cited in: Adv Mater. 2025 Aug;37(32):e2504050. [Abstract]

The phosphorylation levels of EGFR-downstream substrates in H1975^OE cells treated without (Control) or with 500 nM AP-CRTAC^EGFR for 24 h, followed by 6 h of exposure to various concentrations of Osimertinib (Osi). The results showed that AP-CRTAC^EGFR effectively enhanced the efficacy of Osimertinib in inhibiting the phosphorylation of downstream signaling proteins.

Osimertinib mesylate purchased from MedChemExpress. Usage Cited in: Adv Mater. 2025 Aug;37(32):e2504050. [Abstract]

Osimertinib (5 mg/kg; i.g.; once every two days for 14 days) monotherapy did not markedly inhibit tumor growth or reduce tumor weight in patient‑derived xenograft (PDX) mice, whereas combination treatment with AP-CRTAC^EGFR (80 nM/kg; i.t.; once every two days for 14 days) plus Osimertinib significantly suppressed tumor growth and decreased tumor weight.
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.
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
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
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

Osimertinib mesylate purchased from MedChemExpress. Usage Cited in: Cancer Res. 2025 Feb 1;85(3):585-601. [Abstract]

T-cell–mediated tumor cell killing assay of LLC co-mutant cell models treated with Osimertinib (1 μmol/L) or αPD-1 antibody alone or in combination (5 μg/mL). The tumor cells were cocultured with activated T cells for 72 hours. The remaining viable cells were stained with crystal violet. The results showed, compared with single treatment, Egfr/Trp53 and Egfr/Cdkn2a cells showed more sensitivity to the combination treatment of EGFR-TKI (Osimertinib) and PD-1 mAb.

Osimertinib mesylate purchased from MedChemExpress. Usage Cited in: Cancer Res. 2025 Feb 1;85(3):585-601. [Abstract]

T-cell–mediated tumor cell killing assay of LLC-Em cells. Cells were treated with or without anti–PD-L2 antibody, were given Osimertinib (1 μmol/L), selumetinib (1 μmol/L), and Osimertinib + selumetinib, respectively, and then cocultured with activated T cells for 72 hours. IFNγ secreted by CD8⁺ T cells was analyzed by flow cytometry.

Osimertinib mesylate purchased from MedChemExpress. Usage Cited in: Cancer Res. 2025 Feb 1;85(3):585-601. [Abstract]

Tumor-bearing mice were treated with saline, Osimertinib (10 mg/kg), and ZU (100 mg/kg) intragastrically 5 times per week. Mouse anti-CD8 antibody was administered for four consecutive days on days 5 and 12 at 200 μg per mouse via i.p. injection. The models were divided into solvent groups, Osimertinib groups, small-molecule inhibitors ZU, and Osimertinib ZU combined administration groups, and ZU combined administration accompanied CD8⁺ T-cell depletion. Curves showing the tumor volumes from mice in the different groups (n = 6). The results showed that compared with the control treatment, combined Osimertinib and ZU administration significantly inhibited the growth of ectopic tumors, with the inhibition rate reaching 84.9%, but the antitumor effect of the combined treatment was obviously reduced when a CD8 blocking antibody was present.
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

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
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
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

Osimertinib mesylate purchased from MedChemExpress. Usage Cited in: Drug Resist Updat. 2026 May:86:101379. [Abstract]

Photographs of Osimertinib-resistant mouse models and tumors on the 28th day (n = 5 per group). Nude mice were subcutaneously injected with Osimertinib-resistant PC-9 cells. When the tumors were formed, the mice were intratumorally injected with sh-NC/sh-STAB1 macrophages, and treated with vehicle or 5 mg/kg Osimertinib by oral gavage once daily for 28 days.
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

Osimertinib mesylate purchased from MedChemExpress. Usage Cited in: Nat Commun. 2026 Feb 24;17(1):3113. [Abstract]

Western blot analysis of IBI334 and Osimertinib in NCI-H1975^LTC cells (n = 2 biological replicates). For Western blot analysis, cells were treated with 50 nM Osimertinib and/or 100 nM IBI334 for 4 h.
Nat Commun

An alternative EGFR activation by patient-derived R252C mutation promotes cancer progression. [Abstract]

2026 Jan 21;17(1):1902. PMID: 41565660
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
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
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

Osimertinib mesylate purchased from MedChemExpress. Usage Cited in: Redox Biol. 2026 Jun:93:104172. [Abstract]

Cell viability following 48 h treatment with Osimertinib (1 μM) was measured using MTT assays.
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

Osimertinib mesylate purchased from MedChemExpress. Usage Cited in: Mol Cell. 2025 Mar 21:S1097-2765(25)00194-7. [Abstract]

PC9 cell proliferation assay in 100 nM Osimertinib for the indicated conditions, normalized to treatment day 1. n=2 biological replicates. The results showed that PC9 cells expressing NKX2-1 exhibited a reduced maximum killing at day 10 with Osimertinib treatment, and cells specifically increased proliferation by day 17.
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
Genes Dis

2026 Feb 28.
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).
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
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 Sep;12(33):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]

2025 Feb;12(6):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
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
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
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
J Control Release

Macropinocytosis-targeted peptide-docetaxel conjugate for bystander pancreatic cancer treatment. [Abstract]

2024 Dec:376:829-841. PMID: 39491626
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
Cancer Lett

Identification and characterization of Bufalin as a novel EGFR degrader. [Abstract]

2025 Jul 28:623:217715. 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
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
J Pharm Anal

2026 Jun 3.
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
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
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

AZD9291 inactivates the PRC2 complex to mediate tumor growth inhibition. [Abstract]

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
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
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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
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2025 May 15:S1534-5807(25)00287-4. PMID: 40403724
Oncogene

2026 Aug;45(32):3358-3372. PMID: 42420587
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Amphiregulin drives EGFR-dependent genome stability in colorectal cancer and represents a targetable vulnerability. [Abstract]

2026 Jun 15. PMID: 42298179
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YTHDC2 inhibits the resistance of lung cancer to EGFR-TKI through cuproptosis. [Abstract]

2025 Dec 16. PMID: 41402633
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2025 May;44(19):1400-1414. PMID: 40011576
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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
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2024 Sep;43(37):2781-2794. PMID: 39147880
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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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2023 Nov;52(5):102. PMID: 37681495
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2025 Oct 31;16(1):599. PMID: 41174788
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2025 Dec 5;44(12):116659. PMID: 41351835
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2024 Oct 8;43(10):114812. PMID: 39388352
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2023 Nov 8;115(11):1383-1391. PMID: 37481710
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HMOX1 expression influence the role of macrophage in EGFR-TKI resistance of lung adenocarcinoma. [Abstract]

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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]

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Exploration of novel dihydroquinoxalinone derivatives as EGFRL858R/T790M tyrosine kinase inhibitors for the treatment of non-small-cell lung cancer. [Abstract]

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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
Sci Rep

2026 Jul 20. PMID: 42477403
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USP7-dependent stabilization of FKBP4 contributes to acquired osimertinib resistance through glycolytic remodeling in NSCLC. [Abstract]

2026 Apr 24;16(1):18984. PMID: 42031983
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Brexpiprazole, a Serotonin-Dopamine Activity Modulator, Can Sensitize Glioma Stem Cells to Osimertinib, a Third-Generation EGFR-TKI, via Survivin Reduction. [Abstract]

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Nicotinamide N-methyltransferase promotes drug resistance in lung cancer, as revealed by nascent proteomic profiling. [Abstract]

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Inhibition of CDCP1 by 8-isopentenylnaringenin synergizes with EGFR inhibitors in lung cancer treatment. [Abstract]

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MLL4 Regulates the Progression of Non-Small-Cell Lung Cancer by Regulating the PI3K/AKT/SOX2 Axis. [Abstract]

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METTL16-dependent miR-146b-5p m6A modification remodeling sensitize NSCLC to osimertinib via activating PI3K/AKT signaling. [Abstract]

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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 (Osimertinib) treatment.

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Lösungsmittel & Löslichkeit

In Vitro:

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)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

1.6787 mL

8.3933 mL

16.7867 mL

5 mM

0.3357 mL

1.6787 mL

3.3573 mL

10 mM

0.1679 mL

0.8393 mL

1.6787 mL

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.

Molaritätsrechner

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

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.

Protocol 1

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.

Protocol 2

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.

Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: ≥ 1.39 mg/mL (2.33 mM); Clear solution

This protocol yields a clear solution of ≥ 1.39 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (13.9 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
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

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (286 KB)
SDS (393 KB)
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- Portuguese - PT (393 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[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]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

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

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Keywords

Osimertinib mesylate

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Osimertinib mesylate

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