| NT157IRS-1/2 inhibitor, inhibits IGF-1R and STAT3 signaling pathway |
Sample solution is provided at 25 µL, 10mM.
Quality Control & MSDS
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- Purity = 98.41%
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| Cas No. | 1384426-12-3 | SDF | Download SDF |
| Synonyms | N/A | ||
| Chemical Name | (E)-3-(3-bromo-4,5-dihydroxyphenyl)-N-(3,4,5-trihydroxybenzyl)prop-2-enethioamide | ||
| Canonical SMILES | OC1=C(O)C=C(/C=C/C(NCC2=CC(O)=C(O)C(O)=C2)=S)C=C1Br | ||
| Formula | C16H14BrNO5S | M.Wt | 412.26 |
| Solubility | ≥50mg/mL in DMSO | Storage | Store at -20°C |
| Physical Appearance | A solid | Shipping Condition | Evaluation sample solution : ship with blue ice.All other available size:ship with RT , or blue ice upon request |
| General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months. | ||
IC50: 0.3 to 0.8 μM
NT157 is an IRS-1/2 inhibitor.
Insulin receptor substrates 1 and 2 (IRS1/2) mediate antiapoptotic and mitogenic signaling from insulin receptor (IR), insulin-like growth factor 1 receptor (IGF-IR), and other oncoproteins. IRS1 plays a critical role in cancer cell proliferation, and its expression is increased in many human malignancies.
In vitro: NT157 treatment was fonund to be able to lead to dose-dependent suppression of IRS protein expression, inhibition of IGF1R activation, inhibition of IGF1-induced AKT activation, but increased ERK activation in NT157-treated cells. These effects were associated with decreased proliferation, increased apoptosis of LNCaP cells and increased G2-M arrest in PC3 cells. Moreover, NT157 could significantly affect the cell migratory ability, as demonstrated by a wound-healing assay. In addition, the NT157 treatment was able to induce cell cycle arrest and inhibit IGF system signaling [1].
In vivo: In previous animal study, NT157 was found to suppress androgen-responsive growth, delay CRPC progression of LNCaP xenografts, and suppress PC3 tumor growth alone or in combination with docetaxel. This study reported the first preclinical proof-of-principle data that NT157 suppressed IRS1/2 expression, delayed CRPC progression, and suppressed growth of CRPC tumors in vivo [1].
Clinical trial: Up to now, NT157 is still in the preclinical development stage.
Reference:[1] 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.
