Osimertinib mesylate

製品コードS5078 バッチS507801

印刷

化学情報

Chemical Structure Synonyms AZD9291 mesylate Storage
(From the date of receipt)		 3 years -20°C powder
化学式

C29H37N7O5S
分子量 595.71 CAS No. 1421373-66-1
Solubility (25°C)* 体外 DMSO 9 mg/mL (15.1 mM)
 
 
* <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.

溶剤液（一定の濃度）を調合する

生物活性

製品説明 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.
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.

プロトコル(参考用のみ)

細胞アッセイ 細胞株 lung adenocarcinoma (LUAD) cell lines
濃度 0.001 -1 µM
反応時間 72 h
実験の流れ

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.
動物実験 動物モデル BALB/c nu/nu mice bearing PC9, PC9-GR and PC9-OR cells
投薬量 30 mg/kg
投与方法 p.o.

Selleckの高級品が、幾つかの出版された研究調査結果（以下を含む）で使われた：

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

長期の保管のために-20°Cの下で製品を保ってください。

人間や獣医の診断であるか治療的な使用のためにでない。

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