NT157

製品コードS8228 バッチS822801

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

C16H14BrNO5S
分子量 412.26 CAS No. 1384426-12-3
Solubility (25°C)* 体外 DMSO 82 mg/mL (198.9 mM)
Ethanol 82 mg/mL (198.9 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 40%PEG300 5%Tween80 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。

 10.000mg/ml (24.26mM) Taking the 1 mL working solution as an example, add 50 μL of 200 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 500 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 選択的IRS-1/2（インスリン受容体基質）阻害剤であるNT157は、TMEのがん細胞および間質細胞におけるIGF-1RおよびSTAT3シグナル伝達経路を阻害し、がん細胞の生存率を低下させる可能性があります。
in vitro

NT157 treatment resulted in dose-dependent inhibition of IGF1R activation, suppression of IRS protein expression, inhibition of IGF1-induced AKT activation, but increased ERK activation in this compound-treated cells in vitro. These effects were correlated with decreased proliferation and increasing apoptosis of LNCaP cells and increasing G2-M arrest in PC3 cells. This chemical can mediate suppression of IGF1R-mediated survival signaling through the established mechanism for negative feedback of IGF1R signaling: targeting IRS1/2 for serine phosphorylation and subsequent degradation. It displayed little to no effect on the survival of normal melanocytes and fibroblasts.
in vivo

NT157 suppressed androgen-responsive growth, delayed CRPC progression of LNCaP xenografts, and suppressed PC3 tumor growth alone and in combination. Melanoma tumor growth and metastasis is efficiently inhibited by this compound.

プロトコル(参考用のみ)

細胞アッセイ 細胞株 LNCaP cells, PC3 cells
濃度 0-10 μM
反応時間 72 h
実験の流れ Cells were plated in 24-well plates and treated with varying doses of NT157. Crystal violet staining was carried out for time course, and 72 hours after treatment. The absorbance was determined with a microtiter plate reader at 562 nm. Cell survival after this compound treatment was calculated as the percentage of the absorbance in vehicle-treated cells.
動物実験 動物モデル Athymic nude mice (Harlan Sprague-Dawley)
投薬量 50 mg/kg
投与方法 i.p.

参考

  • https://pubmed.ncbi.nlm.nih.gov/25267499/
  • https://pubmed.ncbi.nlm.nih.gov/23651636/

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：

A heterodimer of hemoglobin identifies theranostic targets on brain-metastasizing melanoma cells [ Int J Cancer, 2025, 10.1002/ijc.35458] PubMed: 40285526
Insulin receptor substrate 1 is a novel member of EGFR signaling in pancreatic cells [ Eur J Cell Biol, 2024, 103(4):151457] PubMed: 39326351
ASPSCR1::TFE3-mediated upregulation of insulin receptor substrate 2 (IRS-2) activates PI3K/AKT signaling and promotes malignant phenotype [ Int J Biochem Cell Biol, 2024, 176:106676] PubMed: 39419345
RAGE inhibition blunts insulin-induced oncogenic signals in breast cancer [ Breast Cancer Res, 2023, 25(1):84] PubMed: 37461077
ERα/PR crosstalk is altered in the context of the ERα Y537S mutation and contributes to endocrine therapy-resistant tumor proliferation [ NPJ Breast Cancer, 2023, 9(1):96] PubMed: 38036546
Repressing IRS1/2 by NT157 inhibits the malignant behaviors of ovarian cancer through inactivating PI3K/AKT/mTOR pathway and inducing autophagy [ Kaohsiung J Med Sci, 2023, 10.1002/kjm2.12652] PubMed: 36727938
LRG1 is a novel HER3 ligand to promote growth in colorectal cancer [ bioRxiv, 2023, PPR618443 ] PubMed: none
Endocrine Therapy Resistance-Associated ERα-Y537S Mutation Alters ERα/PR Crosstalk in Breast Cancer [ ProQuest, 2023, ] PubMed: none
Targeting IRS-1/2 in Uveal Melanoma Inhibits In Vitro Cell Growth, Survival and Migration, and In Vivo Tumor Growth [ Cancers (Basel), 2022, 14(24)6247] PubMed: 36551732
MPA alters metabolic phenotype of endometrial cancer-associated fibroblasts from obese women via IRS2 signaling [ PLoS One, 2022, 17(7):e0270830] PubMed: 35816477

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。