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| Cas No.: | 1384426-12-3 |
| Synonyms: | NT157,NT 157 |
| SMILES: | C1=C(C=C(C(=C1O)O)O)CN/C(=C/C=C/2\C=C(C(=O)C(=C2)Br)O)/S |
| Formula: | C16H14BrNO5S |
| M.Wt: | 412.26 |
| Purity: | >98% |
| Sotrage: | 2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO |
| Description: | NT157is a selective inhibitor of IRS-1/2, IC50 values at sub-micromolar doses (ranging from 0.3 to 0.8 μM) . |
| Target: | IC50 value: 0.3 to 0.8 μM [1] Target: Insulin receptor |
| 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] |
| In 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] |
| 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. |
MSDS
COA
| LOT NO. | DOWNLOAD |
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| 2018-0101 |
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| 2018-0101 |
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