NT157

Catalog No.S8228 Batch:S822801

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Technical Data

Formula

C16H14BrNO5S
Molecular Weight 412.26 CAS No. 1384426-12-3
Solubility (25°C)* In vitro DMSO 82 mg/mL (198.9 mM)
Ethanol 82 mg/mL (198.9 mM)
Water Insoluble
In vivo (Add solvents to the product individually and in order)
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.
* Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

Preparing Stock Solutions

Biological Activity

Description 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.
Targets
IRS1/2 [2]
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].

Protocol (from reference)

Cell Assay:[1]
  • Cell lines

    LNCaP cells, PC3 cells

  • Concentrations

    0-10 μM

  • Incubation Time

    72 h

  • Method

    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.
Animal Study:[1]
  • Animal Models

    Athymic nude mice (Harlan Sprague-Dawley)

  • Dosages

    50 mg/kg

  • Administration

    i.p.

Selleck's NT157 has been cited by 12 publications

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

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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

NOT FOR HUMAN, VETERINARY DIAGNOSTIC OR THERAPEUTIC USE.