Osimertinib mesylate

製品コードS5078 バッチS507804

印刷

化学情報

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

20 mg/mL (33.57 mM)

Water

Insoluble

Ethanol

Insoluble

体内（毎回新しく調製した物を用意してください）

Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O この製剤はselleckのラボで検証済みです。上記の溶解方法がご要望を満たさない場合、selleckの営業担当までお問い合わせ頂ければ、個別の試験を行います。	1.250mg/ml (2.10mM)	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.
Clear solution	5% DMSO 1 95% Corn oil この製剤はselleckのラボで検証済みです。上記の溶解方法がご要望を満たさない場合、selleckの営業担当までお問い合わせ頂ければ、個別の試験を行います。	0.625mg/ml (1.05mM)	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.

* <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.

参考

https://pubmed.ncbi.nlm.nih.gov/35144642/
https://pubmed.ncbi.nlm.nih.gov/31564718/

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：

CD105 blockade restores osimertinib sensitivity in drug-resistant EGFR-mutant non-small cell lung cancer [ Drug Resist Updat, 2025, 81:101237]	PubMed: 40090182
RBM15 facilitates osimertinib resistance of lung adenocarcinoma through m6A-dependent epigenetic silencing of SPOCK1 [ Oncogene, 2024, 10.1038/s41388-024-03220-z]	PubMed: 39528815
Patient-derived rhabdomyosarcoma cells recapitulate the genetic and transcriptomic landscapes of primary tumors [ iScience, 2024, 27(10):110862]	PubMed: 39319271
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

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。