Osimertinib mesylate

Catalog No.S5078 Batch:S507804

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Technical Data

Formula

C29H37N7O5S
Molecular Weight 595.71 CAS No. 1421373-66-1
Solubility (25°C)* In vitro DMSO 50 mg/mL (83.93 mM)
Water Insoluble
Ethanol Insoluble
In vivo (Add solvents to the product individually and in order)
Clear solution
5% DMSO 95% Corn oil
0.625mg/ml Taking the 1 mL working solution as an example, add 50 μL of 12.5 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results. 
Clear solution
5%DMSO 40%PEG300 5%Tween80 50%ddH2O
1.25mg/ml Taking the 1 mL working solution as an example, add 50 μL of 25 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results. 
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
* Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

Preparing Stock Solutions

Biological Activity

Description Osimertinib mesylate (AZD9291) is the mesylate form of osimertinib, which is an oral, third-generation epidermal growth factor receptor (EGFR) tyrosine kinase inhibitor (TKI) drug.
Targets
EGFR [1]
In vitro

Osimertinib-resistant lung adenocarcinoma (LUAD) cells express higher level of METTL7B in comparison to Osimertinib-sensitive cells. Knock-down of METTL7B by GNC-siRNA re-sensitized LUAD cells to osimertinib.[1]
In vivo

METTL7B is significantly increased in both mRNA and protein level in osimertinib -resistant xenografts as compared with those in osimertinib-sensitive xenografts. In LUAD CDX mouse model, combination treatment with GNC-siMETTL7B (6 mg siRNA per mouse equivalent) significantly suppresses tumor growth as compared with treatment of osimertinib (30 mg/kg) alone.

Protocol (from reference)

Cell Assay:

[1]
  • Cell lines

    lung adenocarcinoma (LUAD) cell lines

  • Concentrations

    0.001 -1 µM

  • Incubation Time

    72 h

  • Method

    Cells are plated at a density of 3,000 cells/well in 96 well plates. Osimertinib is added to the medium and treated for 72 h. Cell viability assays are performed by Cell Counting Kit-8.

Selleck's Osimertinib mesylate has been cited by 107 publications

Silent mutations reveal therapeutic vulnerability in RAS Q61 cancers [ Nature, 2022, 603(7900):335-342] PubMed: 35236983
Methyltransferase like 7B is a potential therapeutic target for reversing EGFR-TKIs resistance in lung adenocarcinoma [ Mol Cancer, 2022, 21(1):43] PubMed: 35144642
Creating MHC-restricted neoantigens with covalent inhibitors that can be targeted by immune therapy [ Cancer Discov, 2022, CD-22-1074] PubMed: 36250888
Small-molecule targeted therapies induce dependence on DNA double-strand break repair in residual tumor cells [ Sci Transl Med, 2022, 14(638):eabc7480] PubMed: 35353542
Neurokinin-1 receptor promotes non-small cell lung cancer progression through transactivation of EGFR [ Cell Death Dis, 2022, 13(1):41] PubMed: 35013118
c-FLIP promotes drug resistance in non-small-cell lung cancer cells via upregulating FoxM1 expression [ Acta Pharmacol Sin, 2022, 10.1038/s41401-022-00905-7] PubMed: 35422085
A Self-Assembly ICG Nanoparticle Potentiating Targeted Photothermal and Photodynamic Therapy in NSCLC [ ACS Biomater Sci Eng, 2022, 8-10:4535-4546] PubMed: 36070516
Potential use of EGFR-targeted molecular therapies for tumor suppressor CYLD-negative and poor prognosis oral squamous cell carcinoma with chemoresistance [ Cancer Cell Int, 2022, 22(1):358] PubMed: 36376983
Combining EGFR-TKI With SAHA Overcomes EGFR-TKI-Acquired Resistance by Reducing the Protective Autophagy in Non-Small Cell Lung Cancer [ Front Chem, 2022, 10:837987] PubMed: 35402377
Early On-Treatment Prediction of the Mechanisms of Acquired Resistance to EGFR Tyrosine Kinase Inhibitors [ Cancers (Basel), 2022, 14(6)1512] PubMed: 35326664

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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

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