GSK1838705A

  • 化学数据
CAS号 1116235-97-2 货号 BCP02847
中文名 GSK1838705A
英文名 GSK1838705A
中文别名
英文别名 GSK 1838705A;GSK-1838705A;
分子式 C27H29FN8O3 分子量 532.57
  • 用途
生物活性 GSK1838705A potently and ATP-competitively inhibits IGF-1R and IR with appKi values of 0.7 nM and 1.1 nM, respectively.In cells, GSK1838705A potently inhibits ligand-induced phosphorylation of IGF-1R and IR with IC50 of 85 nM and 79 nM, respectively. GSK1838705A shows the significant anti-proliferative effect in a panel of cell lines derived from solid and hematologic tumors such as L-82, SUP-M2, SK-ES and MCF-7 cells with EC50 of 24 nM, 28 nM, 141 nM and 203 nM, respectively. GSK1838705A shows an accumulation of MCF-7 and NCl-H929 cells predominantly in G1 (2N) phase of the cell cycle. GSK1838705A also inhibits ALK with Ki of 0.35 nM and supresses the proliferation of nucleophosmin (NPM)-ALK fusion cells with EC50 of 24-88 nM. GSK1838705A potently inhibits NPM-ALK phosphorylation in Karpas-299 and SR-786 cells, while has modest effect on STAT3 phosphorylation.
信号通路 Angiogenesis/Protein Tyrosine Kinase 
靶 点 Insulin Receptor IGF1R ALK 

结构式

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