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Synonyms | AZD9291 mesylate | Storage (From the date of receipt) |
3 years -20°C powder | |
化学式 | C29H37N7O5S |
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分子量 | 595.71 | CAS No. | 1421373-66-1 | |
Solubility (25°C)* | 体外 | DMSO | 3 mg/mL (5.03 mM) | |
Water | Insoluble | |||
Ethanol | Insoluble | |||
* <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. |
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. |
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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. |
細胞アッセイ | 細胞株 | lung adenocarcinoma (LUAD) cell lines |
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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. |
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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. |
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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。
各々の製品のための特定の保管と取扱い情報は、製品データシートの上で示されます。大部分のSelleck製品は、推薦された状況の下で安定です。製品は、推薦された保管温度と異なる温度で、時々出荷されます。長期の保管のために必要とされてそれと異なる温度で、多くの製品は、短期もので安定です。品質を維持するが、夜通しの積荷のために最も経済的な貯蔵状況を用いてあなたの送料を保存する状況の下に、製品が出荷されることを、我々は確実とします。製品の受領と同時に、製品データシートの上で貯蔵推薦に従ってください。