NT157 - 10mM in DMSO , CAS No.1384426-12-3

CAS: 1384426-12-3 Cat. No.: N408053 Molecular Weight: 412.26

GRADE & PURITY 10mM in DMSO

Synonyms

2-​Propenethioamide, 3-​(3-​bromo-​4,​5-​dihydroxyphenyl)​-​N-​[(3,​4,​5-​trihydroxyphenyl)​methyl]​-​, (2E)​-

Storage

Store at -80°C

Shipped In

Dry ice packs + Cold packs

Overview

Information

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.
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. NT157 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 with docetaxel. Melanoma tumor growth and metastasis is efficiently inhibited by NT157.
Cell Data

cell lines：

Concentrations：0-10 μM

Incubation Time：72 h

Powder Purity:≥98%

Specifications

Synonyms

2-​Propenethioamide, 3-​(3-​bromo-​4, ​5-​dihydroxyphenyl)​-​N-​[(3, ​4, ​5-​trihydroxyphenyl)​methyl]​-​, (2E)​-

Specifications & Purity

10mM in DMSO

Biochemical and Physiological Mechanisms

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.

Storage

Store at -80°C

Shipped In

Dry ice packs + Cold packs

This product requires cold chain shipping. Ground and other economy services are not available.

Action Type

INHIBITOR

Product Properties

• ALogP: 3.721
• HBD Count: 6
• Rotatable Bond: 5

Names and Identifiers

• Isomeric SMILES: C1=C(C=C(C(=C1O)O)O)CNC(=S)/C=C/C2=CC(=C(C(=C2)Br)O)O
• Molecular Weight: 412.26
• Reaxy-Rn: 22688869
• Reaxys-RN_link_address: https://www.reaxys.com/reaxys/secured/hopinto.do?context=S&query=IDE.XRN=22688869&ln=

Chemical and Physical Properties

• DMSO(mg / mL) Max Solubility: 82
• DMSO(mM) Max Solubility: 198.9036045
• Water(mg / mL) Max Solubility: ＜1