Molecular Weight(MW): 412.26
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.
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Choose Selective IGF-1R Inhibitors
|Description||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.|
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.|
|In vitro||DMSO||82 mg/mL (198.9 mM)|
|Ethanol||82 mg/mL (198.9 mM)|
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