Naquotinib(ASP8273)

製品コードS8412 バッチS841201

印刷

化学情報

Chemical Structure 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.
* <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) is an orally available, irreversible, mutant-selective, epidermal growth factor receptor (EGFR) inhibitor, with potential antineoplastic activity.
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, it is evaluated against EGFR mutants (L858R, exon 19 deletion, L858R/T790M, and del19/T790M) and WT EGFR. This compound 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. It even shows activity in mutant EGFR cell line which is resistant to other EGFR TKIs including AZD9291 and CO-1686[1][2].
in vivo In mouse xenograft studies, Naquotinib (ASP8273) 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 its efficacy. In HCC827 and NCI-H1975 xenograft models, it induces tumor regression at 10, 30 and 100mg/kg without affecting body weight. This compound also produces tumor growth inhibition from 10mg/kg in the NSCLC patient derived tumor xenograft, LU1868 which express T790M/L858R. On the other hand, it does not produce significant tumor growth inhibition at 10 and 30mg/kg in A431 xenograft model[1][2].

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

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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