IGF-1R


IGF-1 (The insulin-like growth factor 1) receptor is a protein found on the surface of human cells. It is a transmembrane receptor that is activated by a hormone called insulin-like growth factor 1 (IGF-1) and by a related hormone called IGF-2. It belongs to the large class of tyrosine kinase receptors. This receptor mediates the effects of IGF-1, which is a polypeptide protein hormone similar in molecular structure to insulin. IGF-1 plays an important role in growth and continues to have anabolic effects in adults - meaning that it can induce hypertrophy of skeletal muscle and other target tissues. IGF-1 binds to at least two cell surface receptors: the IGF1 Receptor (IGFR), and the insulin recepto
  • GSK1904529A EY1758

    GSK1904529A是IGF-1R和IR的选择性抑制剂,IC50分别为27 nM和25 nM,对Akt1/2,Aurora A/B,B-Raf,CDK2,EGFR的抑制性相对较弱。

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  • BMS-536924 EY1321

    BMS-536924是一种ATP竞争性的IGF-1R抑制剂,IC50为100 nM,对Mek, Fak,和Lck也具有适中的抑制活性,但对Akt1,和MAPK1/2几乎无抑制活性。

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  • NVP-ADW742 EY1152

    NVP-ADW742是IGF-1R选择性抑制剂,IC50为170nM,比对InsR的抑制性强16倍,对HER2,PDGFR,VEGFR-2,Bcr-Abl和c-Kit活性极低。

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  • PQ 401 EY0290

    PQ 401抑制IGF-1R区域自磷酸化,IC50为低于1 μM。

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