Bioactivity | NT157 (Tyrphostin NT157) is a selective IRS-1/2 inhibitor that induces Ser-phosphorylation and consequently the degradation of IRS-1/2. NT157 (Tyrphostin NT157) is a first-in-class anti-cancer agent that also targets Stat3 signaling pathway[1][2]. | ||||||||||||
Target | IRS-1/2; Stat3 | ||||||||||||
Invitro | NT157 (0.3-3 μM; 72 hours) shows a strong dose-dependent inhibition of growth in all cell lines tested, and the IC50 s ranges from 0.3 to 0.8 μM[1].NT157 (1-3 μM; 24 hours) induces cell cycle arrest in MG-63 and U-2OS OS cells[1].NT157 (1-3 μM; 48 hours) downregulates the Tyr-phosphorylation of IRS-1 in the MG-63 and U-2OS cells[1]. MCE has not independently confirmed the accuracy of these methods. They are for reference only. 0 --> NT157 相关抗体: Cell Proliferation Assay[1] Cell Line: | ||||||||||||
In Vivo | NT157 (50 mg/kg; i.p.; three times per week for 6 weeks) significantly delayed tumor growth in castrated mice bearing LNCaP xenografts [3]. MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: | ||||||||||||
CAS | 1384426-12-3 | ||||||||||||
Formula | C16H14BrNO5S | ||||||||||||
Molar Mass | 412.26 | ||||||||||||
Appearance | 固体 | ||||||||||||
Transport | Room temperature in continental US; may vary elsewhere. | ||||||||||||
Storage |
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Reference | [1]. Downregulated the Tyr-phosphorylation of IRS-1 in the MG-63 and U-2OS cells. [2]. Flashner-Abramson E, et al. Targeting melanoma with NT157 by blocking Stat3 and IGF1R signaling. Oncogene. 2016 May 19;35(20):2675-80. [3]. 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. [4]. 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. |