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    1. Protein Tyrosine Kinase/RTK
    2. IGF-1R


    IGF-1R (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. Mice carrying only one functional copy of IGF-1R are normal, but exhibit a ~15% decrease in body mass. The IGF-1R is implicated in several cancers, including breast, prostate, and lung cancers. In some instances its anti-apoptotic properties allow cancerous cells to resist the cytotoxicproperties of chemotherapeutic drugs or radiotherapy.

    IGF-1R 相关产品 (19):

    Cat. No. Product Name Effect Purity
    • HY-10191
      Linsitinib Inhibitor 99.90%
      Losmapimod是 IGF-1胰岛素受体的双重抑制剂,IC50 分别为35 和 75 nM。
    • HY-15656
      Ceritinib Inhibitor 99.97%
      Ceritinib (LDK378) 是有效且特异性的 ALK 抑制剂,IC50 为 0.2 nM。
    • HY-15494
      Picropodophyllin Inhibitor 99.58%
      Picropodophyllin (AXL1717) 是选择性的胰岛素样生长因子-1受体 (IGF-1R)抑制剂,IC50 为1 nM。
    • HY-10200
      BMS-754807 Inhibitor 99.18%
      BMS-754807 是有效、可逆的胰岛素样生长因子1受体/胰岛素受体抑制剂,其 IC50 值分别为 1.8 和 1.7 nM,Ki 值均小于 2 nM;同时也抑制 Met,RON,TrkA,TrkB,AurA 和 AurB 的活性,其IC50 值分别为 6,44,7,4,9和 25 nM。
    • HY-50866
      NVP-AEW541 Inhibitor 98.76%
      NVP-AEW541 是一种有效的 IGF-1R 抑制剂,IC50 为 0.15 μM,也抑制 InsRIC50 为 0.14 μM。
    • HY-15609
      AZD-3463 Inhibitor 98.49%
    • HY-10262
      BMS-536924 Inhibitor 98.73%
      BMS-536924是ATP竞争性IGF-1R/IR抑制剂, IC50分别为100 nM/73 nM。
    • HY-13020
      GSK1838705A Inhibitor 98.99%
      GSK1838705A是高效,可逆的 IGF-IR 和胰岛素受体 (insulin receptor) 抑制剂,IC50 值分别为2.0 和 1.6 nM。也可抑制 ALKIC50 值为0.5 nM。
    • HY-15749
      XL228 Inhibitor 99.58%
      XL228是多靶点的酪氨酸激酶抑制剂,对Bcr-AblAurora AIGF-1RSrcLynIC50 值分别为5,3.1,1.6,6.1,2 nM。
    • HY-15656A
      Ceritinib dihydrochloride Inhibitor 99.86%
      Ceritinib dihydrochloride (LDK378 dihydrochloride) 是 ALK 抑制剂,IC50 为 0.2 nM,比对 IGF-1R 和 InsR 的抑制性高 40 倍和 35 倍。
    • HY-10252
      NVP-ADW742 Inhibitor 99.66%
      NVP-ADW742(ADW742; GSK 552602A )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。
    • HY-B0794A
      AZ7550 hydrochloride Inhibitor 98.02%
      AZ7550 hydrochloride 是 AZD9291 的一种活性代谢物,AZ7550 抑制 IGF1R 活性,IC50 为 1.6 μM。
    • HY-10253
      AG1024 Inhibitor
      AG-1024 (Tyrphostin)能抑制IGF-1R自磷酸化,IC50为7 μM,而对IR的IC50则为57 μM。
    • HY-N0908
      Ginsenoside Rg5 Agonist 99.36%
      Ginsenoside Rg5 是红参的主要成分。Ginsenoside Rg5 阻断 IGF-1 与其受体的结合,IC50 约为90 nM。Ginsenoside Rg5 还通过抑制 NF-κB p65 的 DNA 结合活性来抑制 COX-2 的 mRNA 表达。
    • HY-10524
      GSK1904529A Inhibitor 98.97%
      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。
    • HY-B0794B
      AZ7550 Mesylate Inhibitor 98.85%
      AZ7550 Mesylate 是 AZD9291 的一种活性代谢物,AZ7550 抑制 IGF1R 活性,IC50 为 1.6 μM。
    • HY-13686
      PQ401 Inhibitor 98.59%
      PQ401是IGF1R阻断剂,能抑制IGF1R自磷酸化,IC50 < 1 uM。
    • HY-B0794
      AZ7550 Inhibitor
      AZ7550 是 AZD9291 的一种活性代谢物,AZ7550 抑制 IGF1R 活性,IC50 为 1.6 μM。
    • HY-18785
      Indirubin Derivative E804 Inhibitor
      Indirubin Derivative E804, 是类胰岛素生长因子1型受体 (IGF1R) 的有效抑制剂,其 IC50 值为 0.65 μM。
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