GSK 1838705

Biological Activity

GSK 1838705 is a 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

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.

Additional Information

Background References

1. GSK1838705A inhibits the Ins-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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