| CAS NO: | 1384426-12-3 |
| 包装 | 价格(元) |
| 2mg | 电议 |
| 5mg | 电议 |
| 25mg | 电议 |
| Cas No. | 1384426-12-3 |
| 化学名 | (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 |
| 分子式 | C16H14BrNO5S |
| 分子量 | 412.26 |
| 溶解度 | ≥ 50mg/mL in DMSO |
| 储存条件 | Store at -20℃ |
| General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while. |
| Shipping Condition | Evaluation sample solution : ship with blue ice All other available size: ship with RT , or blue ice upon request |
| 产品描述 | 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: |
m.cnreagent.com