Cat. No. 5111
Chemical Name: 2-[[2-[[1-[(Dimethylamino)ethanoyl]
Biological ActivityPotent 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.
Licensing InformationSold for research purposes under agreement from GlaxoSmithKline.
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.
Certificate of Analysis / Product Datasheet / Safety Datasheet
References are publications that support the products' biological activity.
Gao et al (2014) Site-specific activation of AKT protects cells from death induced by glucose deprivation. Oncogene 33 745. PMID: 23396361.
Chamberlain et al (2009) Optimization of 4,6-bis-anilino-1H-pyrrolo[2,3-d]pyrimidine IGF-1R tyrosine kinase inhibitors towards JNK selectivity. Bioorg.Med.Chem.Lett. 19 360. PMID: 19071018.
Sabbatini et al (2009) GSK1838705A inhibits the insulin-like growth factor-1 receptor and anaplastic lymphoma kinase and shows antitumor activity in experimental models of human cancers. Mol.Cancer.Ther. 8 2811. PMID: 19825801.
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