Home Protein Tyrosine Kinase IGF-1R inhibitor NT157 For research use only.

NT157

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.

NT157 Chemical Structure

NT157 Chemical Structure

CAS: 1384426-12-3

Selleck's NT157 has been cited by 12 publications

Purity & Quality Control

Batch: S822801 DMSO] 82 mg/mL] false] Ethanol] 82 mg/mL] false] Water] Insoluble] false Purity: 98.91%
98.91

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Signaling Pathway

IGF-1R Signaling Pathways

IGF-1R Signaling Pathway

Choose Selective IGF-1R Inhibitors

Cell Data

Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
KB-8-5-11 qHTS assay P-glycoprotein substrates identified in KB-8-5-11 adenocarcinoma cell line, qHTS therapeutic library screen, Potency = 7.3078 μM. 31515284
KB-3-1 qHTS assay P-glycoprotein substrates identified in KB-3-1 adenocarcinoma cell line, qHTS therapeutic library screen 31515284
Click to View More Cell Line Experimental Data

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
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].
Cell Research 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.
Experimental Result Images Methods Biomarkers Images PMID
Western blot IRS-1 / IRS-2 p-IRS1 / p-AKT / AKT / p-S6 / S6 / Shc / p-ERK / ERK 26029165
Growth inhibition assay Cell viability 26029165
In Vivo
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].
Animal Research Animal Models Athymic nude mice (Harlan Sprague-Dawley)
Dosages 50 mg/kg
Administration i.p.

Chemical Information & Solubility

Molecular Weight 412.26 Formula

C16H14BrNO5S
CAS No. 1384426-12-3 SDF Download NT157 SDF
Smiles C1=C(C=C(C(=C1O)O)O)CNC(=S)C=CC2=CC(=C(C(=C2)Br)O)O
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 82 mg/mL ( (198.9 mM)； Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 82 mg/mL

Water : Insoluble


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In vivo
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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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