Naquotinib(ASP8273)

製品コードS8412 バッチS841201

印刷

化学情報

Synonyms

N/A

Storage
(From the date of receipt)

3 years -20°C powder
1 years -80°C in solvent

化学式

C₃₀H₄₂N₈O₃

分子量

562.71

CAS No.

1448232-80-1

Solubility (25°C)*

体外

Ethanol (warmed with 50ºC water bath)

100 mg/mL (177.71 mM)

DMSO (warmed with 50ºC water bath)

52 mg/mL (92.4 mM)

Water

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。	2.6mg/ml (4.62mM)	Taking the 1 mL working solution as an example, add 50 μL of 52 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。	0.175mg/ml (0.31mM)	Taking the 1 mL working solution as an example, add 50 μL of 3.5 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	Naquotinib (ASP8273) は、経口投与可能で不可逆的な変異型選択的上皮成長因子受容体 (EGFR) 阻害剤であり、抗腫瘍活性を有する可能性があります。
in vitro	Naquotinib (ASP8273) is a small-molecule irreversible TKI inhibitor that inhibits the kinase activity of EGFR mutations including T790M, with limited activity against EGFR wild-type (WT) NSCLC. In the in vitro enzymatic and cell-based assays, this compound is evaluated against EGFR mutants (L858R, exon 19 deletion, L858R/T790M, and del19/T790M) and WT EGFR. It is found by mass spectrometry to covalently bind to a mutant EGFR (L858R/T790M) via cysteine residue 797 in the kinase domain of EGFR with long-lasting inhibition of EGFR phosphorylation for 24 h. In the NSCLC cell lines harboring the above EGFR mutations, it has IC50 values of 8-33 nM toward EGFR mutants, more potently than that of WT EGFR (IC50 value of 230 nM). It is further shown to suppress the signaling pathway through ERK and Akt. This compound even shows activity in mutant EGFR cell line which is resistant to other EGFR TKIs including AZD9291 and CO-1686.
in vivo	In mouse xenograft studies, S8412 induces tumor regression in NCI-H1975 (L858R/T790M), HCC827 (del ex19) and PC-9 (del ex19) xenograft models by repeated oral dosing in a dose-dependent manner. Dosing schedules do not affect the efficacy of ASP8273. In HCC827 and NCI-H1975 xenograft models, S8412 induces tumor regression at 10, 30 and 100mg/kg without affecting body weight. S8412 also produces tumor growth inhibition from 10mg/kg in the NSCLC patient derived tumor xenograft, LU1868 which express T790M/L858R. On the other hand, S8412 does not produce significant tumor growth inhibition at 10 and 30mg/kg in A431 xenograft model.

プロトコル(参考用のみ)

参考

http://cancerres.aacrjournals.org/content/74/19_Supplement/1728.short
http://cancerres.aacrjournals.org/content/75/15_Supplement/2586.short

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：

Emerging drugs for EGFR-mutated non-small cell lung cancer [Sukrithan V, et al. Expert Opin Emerg Drugs, 2018, 10.1080/14728214.2018.1558203 Share on FacebookShare on TwitterShare on Google+]	PubMed: 30570396

Emerging drugs for EGFR-mutated non-small cell lung cancer [Sukrithan V, et al. Expert Opin Emerg Drugs, 2018, 10.1080/14728214.2018.1558203 Share on FacebookShare on TwitterShare on Google+]

PubMed: 30570396

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。