SGI-7079

製品コードS7847 バッチS784701

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

C26H26FN7
分子量 455.53 CAS No. 1239875-86-5
Solubility (25°C)* 体外 DMSO 91 mg/mL (199.76 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.
* <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 SGI-7079 ,a novel selective Axl inhibitor, inhibits tumor growth in a dose dependent manner and is a potential therapeutic target for overcoming EGFR inhibitor resistance.
in vitro SGI-7079 exhibits a Ki = 5.7 nM for AXL and inhibits Gas6 ligand-induced tyrosine phosphorylation of human AXL expressed in HEK293T cells (EC50 = 100 nM). It inhibits TAM family members MER and Tyro3 similarly as AXL, and shows potent, low nM inhibition of Syk, Flt1, Flt3, Jak2, TrkA, TrkB, PDGFRβ and Ret kinases. Mesenchymal cells express increased levels of the receptor tyrosine kinase Axl and show a trend toward greater sensitivity to this compound.
in vivo SGI-7079 inhibits tumor growth in a dose-dependent manner, and at the maximum dose, this compound inhibits tumor growth by 67%, compared with control. the combination of this chemical with erlotinib reverses erlotinib resistance in mesenchymal lines expressing Axl and in a xenograft model of mesenchymal NSCLC.

プロトコル(参考用のみ)

細胞アッセイ 細胞株 HEK-293 cells
濃度 0.03, 0.1, 0.3, 1, 3 μmol/L
反応時間 10 min
実験の流れ

To show inhibition of Axl activation by SGI-7079, HEK-293 cells are transiently transfected by electroporation with 1 mg FLAG-tagged plasmid containing the human Axl gene and allowed to incubate in standard media + 10% FBS for 24 hours. Cells are treated with this compound for 10 minutes at the indicated concentrations. Five minutes before lysis, the cells are stimulated with Gas6-containing WI38 conditioned media.
動物実験 動物モデル Mouse(NCr-nu/nu female mice) xenograft model of NSCLC using the mesenchymal NSCLC cell line A549
投薬量 10, 25, 50 mg/kg
投与方法 p.o.

参考

  • https://pubmed.ncbi.nlm.nih.gov/26555154/
  • https://pubmed.ncbi.nlm.nih.gov/23091115/

カスタマーフィードバック

Data from [Data independently produced by , , Oncotarget, 2017, 8(52): 89761–89774 ]

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：

Synergistic Inhibition of Drug Resistant KRAS Mutant Non-Small Cell Lung Cancer by Co-Targeting AXL and SRC [ Cancers (Basel), 2025, 17(3)490] PubMed: 39941857
SIRT3 overexpression and epigenetic silencing of catalase regulate ROS accumulation in CLL cells activating AXL signaling axis [ Blood Cancer J, 2021, 11(5):93] PubMed: 34001853
Integrative Analysis Identifies a Novel AXL-PI3 Kinase-PD-L1 Signaling Axis Associated with Radiation Resistance in Head and Neck Cancer [ Clin Cancer Res, 2017, 23(11):2713-2722] PubMed: 28476872
Axl inhibition induces the antitumor immune response which can be further potentiated by PD-1 blockade in the mouse cancer models. [ Oncotarget, 2017, 8(52):89761-89774] PubMed: 29163786

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。