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）
Clear solution
5%DMSO 40%PEG300 5%Tween80 50%ddH2O
10.0mg/ml 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 NT157, a selective inhibitor of IRS-1/2(insulin receptor substrate), has the potential to inhibit IGF-1R and STAT3 signaling pathways in cancer cells and stroma cells of TME leading to a decrease in cancer cell survival.
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 NT157-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. NT157 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[1]. NT157 displayed little to no effect on the survival of normal melanocytes and fibroblasts[2].
in vivo NT157 suppressed androgen-responsive growth, delayed CRPC progression of LNCaP xenografts, and suppressed PC3 tumor growth alone and in combination with docetaxel[1]. Melanoma tumor growth and metastasis is efficiently inhibited by NT157[2].

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 NT157 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.

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：

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
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
FGFR1 overexpression renders breast cancer cells resistant to metformin through activation of IRS1/ERK signaling [ Biochim Biophys Acta Mol Cell Res, 2021, 1868(1):118877] PubMed: 33007330
Targeting oncogenic mutations in colorectal cancer using cryptotanshinone [ PLoS One, 2021, 16(2):e0247190] PubMed: 33596259
NT157 Inhibits HCC Migration via Downregulating the STAT3/Jab1 Signaling Pathway [ Technol Cancer Res Treat, 2021, 20:15330338211027916] PubMed: 34238066
SQSTM1/p62 Controls mtDNA Expression and Participates in Mitochondrial Energetic Adaption via MRPL12 [ iScience, 2020, 23(8):101428] PubMed: 32805647
Angiotensin-(1-7), the product of ACE2 ameliorates NAFLD by acting through its receptor Mas to regulate hepatic mitochondrial function and glycolipid metabolism [ FASEB J, 2020, 10.1096/fj.202001639R] PubMed: 33078906

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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