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