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GSK1838705A研究進展

發(fā)布日期：2017-11-01   瀏覽次數(shù)：0
核心提示：a href=https://www.medchemexpress.com/GSK1838705A.htmlGSK1838705A/a產(chǎn)品描述：GSK1838705A is a potent small-molecule IGF-
GSK1838705A產(chǎn)品描述：GSK1838705A is a potent small-molecule IGF-1R, the insulin receptor and anaplastic lymphoma kinase (ALK) inhibitor with IC50 of 2.0, 1.6 and 0.5 nM, respectively. IC50 value: 2.0/1.6/0.5 nM ( IGF-1R/InsR/ALK) Target: IGF-1R/InsR/ALKGSK1838705A prevents the in vitro proliferation of cell lines derived from solid and hematologic malignancies, including multiple myeloma and Ewing’s sarcoma, and retards the growth of human tumor xenografts in vivo. Despite the inhibitory effect of GSK1838705A on insulin receptor, minimal effects on glucose homeostasis were obtained at efficacious doses. A single oral dose of GSK1838705A at 0.1 and 0.3 mg/kg led to 35% and 65% prevention of IGF-IR phosphorylation, respectively, wheras doses ≥1 mg/kg led to complete inhibition of ligand-induced IGF-IR phosphorylation. Meanwhile, at a dose of 30 mg/kg, prevention was lasted for  24 hours after compound injection. GSK1838705A also suppresses the anaplastic lymphoma kinase (ALK), which mediates the aber


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