GNF-7

製品コードS8140 バッチS814002

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

C28H24F3N7O2
分子量 547.53 CAS No. 839706-07-9
Solubility (25°C)* 体外 DMSO 20 mg/mL (36.52 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 GNF-7 is a potent type-II kinase Bcr-Abl inhibitor with IC50 of <5 nM, 61 nM, 122 nM, 136 nM, and 133 nM for M351T, T315I, E255 V, G250E, and c-Abl, respectively.
in vitro GNF-7 shows potent antiproliferative activity against wild-type and mutant Bcr-Abl Ba/F3 cells with IC50 less than 11 nM. In human colon cancer cells (Colo205 and SW620), this compound also displays excellent growth inhibitory activity with IC50 of 5 nM and 1 nM, respectively. [1] It potently and selectively inhibits NRAS-dependent acute myelogenous leukemia and acute lymphoblastic leukemia cells through combined inhibition of ACK1/AKT and GCK. [2]
in vivo GNF-7 exhibits excellent pharmacokinetic parameters in mice. In a bioluminescent xenograft mouse model using a transformed T315I-Bcr-Abl-Ba/F3 cell line, this compound (10 mg/kg, p.o.) effectively inhibits tumor growth. [1] In NSG mice bearing human mutant NRAS-expressing MOLT-3-luc+ tumors, this compound (15 mg/kg, p.o.) significantly decreases disease burden, prolongs overall survival, and causes strong suppression of phospho-AKT and phospho-RPS6. [2]

プロトコル(参考用のみ)

動物実験 動物モデル SCID beige female mice bearing T315I-Bcr-Abl-Ba/F3 orthotopic xenografts
投薬量 20 mg/kg
投与方法 p.o.

参考

  • https://pubmed.ncbi.nlm.nih.gov/20604564/
  • https://pubmed.ncbi.nlm.nih.gov/25833960/

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：

PI3K/AKT signaling mediates stress-inducible amyloid formation through c-Myc [ Cell Rep, 2025, 44(5):115617] PubMed: 40272983
The Kinase Inhibitor GNF-7 Is Synthetically Lethal in Topoisomerase 1-Deficient Ewing Sarcoma [ Cancers (Basel), 2025, 17(15)2475] PubMed: 40805174
SH2 domain protein E and ABL signaling regulate blood vessel size [ PLoS Genet, 2024, 20(1):e1010851] PubMed: 38190417
Identification of PARN nuclease activity inhibitors by computational-based docking and high-throughput screening [ Sci Rep, 2023, 13(1):5244] PubMed: 37002320
Identification of PARN nuclease activity inhibitors by computational-based docking and high-throughput screening [ Sci Rep, 2023, 13(1):5244] PubMed: 37002320
SH2 domain protein E (SHE) and ABL signaling regulate blood vessel size [ bioRxiv, 2023, 2023.07.03.547455] PubMed: 37461480
SH2 domain protein E -SHE) and ABL signaling regulate blood vessel size [ bioRxiv, 2023, 2023.07.03.547455] PubMed: 37461480

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。