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
  • Picropodophyllin EY1738

    AXL1717是口服活性的IGF-1R高活性抑制剂,IC50为1 nM,对IR,FGFR,PDGFR和EGFR的抑制性较弱,对微管和DNA拓扑异构酶II无活性。

  • OSI-906 EY1647

    Linsitinib(OSI-906)是口服活性的ATP竞争性IGF-1R和insulin受体双重抑制剂,IC50分别为35 nM和75 nM。

  • BMS-754807 EY1487

    BMS-754807是一种有效的IGF-1R/InsR可逆性抑制剂,IC50为1.8 nM/1.7 nM,对Met, Aurora A/B, TrkA/B和Ron作用稍弱,对Flt3, Lck, MK2, PKA, PKC等几乎没有抑制活性。

  • AG-1024 EY1348

    AG-1024能抑制IGF-1R自磷酸化,IC50为7 μM,而对IR的IC50则为57 μM。

  • NVP-AEW541 EY1355

    NVP-AEW541(AEW-541)是IGF-1R抑制剂,IC50为86 nM,比对InsR的抑制性强27倍。

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