NT157

Catalog No.S8228 Batch:S822802

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
* <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.)

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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^[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.

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.

References

Selleck's NT157 has been cited by 18 publications

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
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
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

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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.