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GSK1904529A

CAS No. : 1089283-49-7

MCE 站：GSK1904529A

产品活性：GSK1904529A 是一种有效的，选择性的，具有口服活性和 ATP 竞争性的胰岛素样生长因子 1 受体 (IGF-1R) 和胰岛素受体 (IR) 抑制剂，IC₅₀ 值分别为 27 和 25 nM。GSK1904529A 在其他 45 种丝氨酸/苏氨酸和酪氨酸激酶中显示出较弱的活性 (IC₅₀>1 μM)。GSK1904529A 具有抗肿瘤活性。

研究领域：Protein Tyrosine Kinase/RTK  |  Apoptosis

作用靶点：IGF-1R  |  Insulin Receptor  |  Apoptosis

In Vitro: GSK1904529A displays high affinities for IGF-1R and IR, with K_is of 1.6 and 1.3 nM, respectively.
GSK1904529A (72 h) inhibits tumor cells proliferation with IC₅₀s ranges from 35 nM to >30 μM, and Ewing's sarcoma and multiple myeloma cell lines are greatest sensitive.
GSK1904529A (0.03-3 μM; 24 and 48 h) arrests cells at the G1 phase of the cell cycle.
GSK1904529A (2 h) inhibits phosphorylation of IGF-IR and IR with IC₅₀s of 22 and 19 nM in NIH-3T3/LISN and NIH-3T3-hIR cells, respectively.
GSK1904529A (0.01-3 μM; 4 h) blocks the major downstream signal transduction pathways mediated by IGF-IR and IR in NIH-3T3/LISN and NIH-3T3-hIR cells.

In Vivo: GSK1904529A (30 mg/kg; p.o. once or twice daily for 21 d) has antitumor activity in mice.
GSK1904529A (1-30 mg/kg; a single p.o.) decreases IGF-I-induced IGF-IR phosphorylation in a dose-dependent manner in mice.
GSK1904529A (30 mg/kg; p.o. once or twice daily for 21 d) has no significant alterations in the blood glucose levels in mice.

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