NT157

Modify Date: 2024-01-31 12:47:04

NT157 Structure
NT157 structure
Common Name NT157
CAS Number 1384426-12-3 Molecular Weight 412.255
Density 1.8±0.1 g/cm3 Boiling Point 660.3±65.0 °C at 760 mmHg
Molecular Formula C16H14BrNO5S Melting Point N/A
MSDS N/A Flash Point 353.1±34.3 °C

 Use of NT157


NT157is a selective inhibitor of IRS-1/2, IC50 values at sub-micromolar doses (ranging from 0.3 to 0.8 μM) .IC50 value: 0.3 to 0.8 μM [1]Target: Insulin receptorin vitro: NT157 significantly affects the cells' migratory ability, as confirmed by a wound-healing assay. NT157 induces cytostatic effects, as evidenced by G2/M cell cycle arrest, and does not affect apoptosis. NT157, a novel small-molecule that specifically targets IRS protein, in OS cells. NT157 is a small-molecule inhibitor that induces Ser-phosphorylation and consequently the degradation of IRS-1 and IRS-2. NT157 efficiently affects migration ability of MG-63 and U-2OS OS cells. NT157 treatment induces cell cycle arrest and inhibits IGF system signaling. [1] The density of LNCaP cells grown in FBS was decreased approximately 20% at 1 μM, approximately 70% at 2 μM, and >90% at 5 μM (IC50, 1.4 μM). Growth of LNCaP cells is suppressed >60% when cultured in CSS but still exhibited significant density at 2 μM and maximal decreased density at 5 μM. The density of FBS-cultured PC3 cells was similarly decreased by NT157 treatment (40% at 2 μM and > 70% at 5 μM; IC50, 2.5 μM). [2]in vivo: NT157 suppresses growth of LNCaP xenografts following castration. NT157 treatment affects IGF1R and IRS targets in xenografts and significantly delays castration-resistant progression of LNCaP androgen-responsive xenografts when combined with castration. NT157 potentiates docetaxel activity in PC3 xenografts.[2]

 Names

Name nt-157
Synonym More Synonyms

 NT157 Biological Activity

Description NT157is a selective inhibitor of IRS-1/2, IC50 values at sub-micromolar doses (ranging from 0.3 to 0.8 μM) .IC50 value: 0.3 to 0.8 μM [1]Target: Insulin receptorin vitro: NT157 significantly affects the cells' migratory ability, as confirmed by a wound-healing assay. NT157 induces cytostatic effects, as evidenced by G2/M cell cycle arrest, and does not affect apoptosis. NT157, a novel small-molecule that specifically targets IRS protein, in OS cells. NT157 is a small-molecule inhibitor that induces Ser-phosphorylation and consequently the degradation of IRS-1 and IRS-2. NT157 efficiently affects migration ability of MG-63 and U-2OS OS cells. NT157 treatment induces cell cycle arrest and inhibits IGF system signaling. [1] The density of LNCaP cells grown in FBS was decreased approximately 20% at 1 μM, approximately 70% at 2 μM, and >90% at 5 μM (IC50, 1.4 μM). Growth of LNCaP cells is suppressed >60% when cultured in CSS but still exhibited significant density at 2 μM and maximal decreased density at 5 μM. The density of FBS-cultured PC3 cells was similarly decreased by NT157 treatment (40% at 2 μM and > 70% at 5 μM; IC50, 2.5 μM). [2]in vivo: NT157 suppresses growth of LNCaP xenografts following castration. NT157 treatment affects IGF1R and IRS targets in xenografts and significantly delays castration-resistant progression of LNCaP androgen-responsive xenografts when combined with castration. NT157 potentiates docetaxel activity in PC3 xenografts.[2]
Related Catalog
References

[1]. Garofalo C, et al. Preclinical Effectiveness of Selective Inhibitor of IRS-1/2 NT157 in Osteosarcoma Cell Lines. Front Endocrinol (Lausanne). 2015 May 13;6:74.

[2]. Ibuki N, et al. The tyrphostin NT157 suppresses insulin receptor substrates and augments therapeutic response of prostate cancer. Mol Cancer Ther. 2014 Dec;13(12):2827-39.

[3]. Ishii H, et al. miR-130a and miR-145 reprogram Gr-1+CD11b+ myeloid cells and inhibit tumor metastasis through improved host immunity. Nat Commun. 2018 Jul 4;9(1):2611.

 Chemical & Physical Properties

Density 1.8±0.1 g/cm3
Boiling Point 660.3±65.0 °C at 760 mmHg
Molecular Formula C16H14BrNO5S
Molecular Weight 412.255
Flash Point 353.1±34.3 °C
Exact Mass 410.977600
PSA 145.27000
LogP 2.89
Vapour Pressure 0.0±2.1 mmHg at 25°C
Index of Refraction 1.811
Storage condition -20°C

 Synonyms

2-Propenethioamide, 3-(3-bromo-4,5-dihydroxyphenyl)-N-[(3,4,5-trihydroxyphenyl)methyl]-, (2E)-
(2E)-3-(3-Bromo-4,5-dihydroxyphenyl)-N-(3,4,5-trihydroxybenzyl)-2-propenethioamide
(E)-3-(3-bromo-4,5-dihydroxyphenyl)-N-(3,4,5-trihydroxybenzyl)prop-2-enethioamide
NT157
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