IDF-11774

製品コードS8771 バッチS877101

印刷

化学情報

 Chemical Structure Synonyms N/A Storage
(From the date of receipt)
3 years -20°C powder
化学式

C23H32N2O2

分子量 368.51 CAS No. 1429054-28-3
Solubility (25°C)* 体外 DMSO 15 mg/mL (40.7 mM)
Ethanol 5 mg/mL (13.56 mM)
Water Insoluble
体内 (毎回新しく調製した物を用意してください)
Clear solution
10%DMSO 40%PEG300 5%Tween80 45%ddH2O
3.0mg/ml Taking the 1 mL working solution as an example, add 100 μL of 30 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 make it clear; then continue to add 450 μL of ddH2O to adjust the volume to 1 mL. 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 IDF-11774 is a hypoxia-inducible factor-1 (HIF-1) inhibitor. It reduces the HRE-luciferase activity of HIF-1α (IC50 = 3.65 μM) and blocks HIF-1α accumulation under hypoxia in HCT116 human colon cancer cells.
in vitro

IDF-11774 inhibits the accumulation of HIF-1α in vitro and in vivo in colorectal carcinoma HCT116 cells under hypoxic conditions. The treatment of IDF-11774 suppresses angiogenesis of cancer cells by reducing the expression of HIF-1 target genes, reduces glucose uptake, thereby sensitizing cells to growth under low glucose conditions, and decreases the extracellular acidification rate (ECAR) and oxygen consumption rate of cancer cells. Therefore, IDF-11774 reduces cancer cell growth through the regulation of cancer glycolytic metabolism and energy production[1].

in vivo

IDF-11774 exhibited substantial anticancer efficacy in mouse models containing KRAS, PTEN, or VHL mutations, which often occur in malignant cancers[1].

プロトコル(参考用のみ)

細胞アッセイ 細胞株 HCT116 cells
濃度 5, 10, 20 μM
反応時間 18 h
実験の流れ

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動物実験 動物モデル Balb/c nude mice bearing tumors (100 mm3) formed from HCT116 cells (1 × 107) expressing HRE-luciferase by subcutaneous injection
投薬量 50 mg/kg
投与方法 p.o.

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:

Targeting APLN/APJ restores blood-testis barrier and improves spermatogenesis in murine and human diabetic models [ Nat Commun, 2022, 13(1):7335] PubMed: 36443325
Staphylococcus aureus Infection Initiates Hypoxia-Mediated Transforming Growth Factor-β1 Upregulation to Trigger Osteomyelitis [ mSystems, 2022, 7(4):e0038022] PubMed: 35852344
Trabectedin induces ferroptosis via regulation of HIF-1α/IRP1/TFR1 and Keap1/Nrf2/GPX4 axis in non-small cell lung cancer cells [ Chem Biol Interact, 2022, 369:110262] PubMed: 36396105
Inhibition of hypoxia-inducible factor-1α alleviates acinar cell necrosis in a mouse model of acute pancreatitis [ Biochem Biophys Res Commun, 2021, 572:72-79] PubMed: 34358966
Secreted frizzled-related protein 2 inhibits the proliferation and metastasis of human colorectal cancer cell line SW480 [ Basic & Clinical Medicine, 2020, 40(9): 1212-1217] PubMed: None

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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