Catalog Number: 5111
Chemical Name: 2-[[2-[[1-[(Dimethylamino)ethanoyl]-5-(methyloxy)-2,3-dihydro-1H-indol-6-yl]amino]-7H-pyrrolo[2,3-d]pyrimidin-4-yl]amino]-6-fluoro-N-methylbenzamide
Biological Activity
Potent insulin receptor (IR) and insulin-like growth factor-1 receptor (IGF1R) inhibitor (IC50 values are 1.6 and 2 nM, respectively). Also inhibits anaplastic lymphoma kinase (ALK) (IC50 = 0.5 nM). Displays > 800-fold selectivity for IR, IGFR1 and ALK over a panel of 44 kinases including JNK. Blocks proliferation of cancer cell lines in vitro, and causes complete regression of ALK-dependent tumors in vivo. Orally bioavailable.
Technical Data
  • M.Wt:
    532.57
  • Formula:
    C27H29FN8O3
  • Solubility:
    Soluble to 100 mM in DMSO
  • Purity:
    >98%
  • Storage:
    Store at -20°C
  • CAS No:
    1116235-97-2
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis. All Tocris products are intended for laboratory research use only.
Additional Information
Licensing Caveats:
Sold for research purposes under agreement from GlaxoSmithKline.
Background References
  1. GSK1838705A inhibits the insulin-like growth factor-1 receptor and anaplastic lymphoma kinase and shows antitumor activity in experimental models of human cancers.
    Sabbatini et al.
    Mol.Cancer.Ther., 2009;8:2811
  2. Site-specific activation of AKT protects cells from death induced by glucose deprivation.
    Gao et al.
    Oncogene, 2014;33:745
  3. Optimization of 4,6-bis-anilino-1H-pyrrolo[2,3-d]pyrimidine IGF-1R tyrosine kinase inhibitors towards JNK selectivity.
    Chamberlain et al.
    Bioorg.Med.Chem.Lett., 2009;19:360

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