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.
Sold for research purposes under agreement from GlaxoSmithKline.
|Storage||Store at -20°C|
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.
|Solvent||Max Conc. mg/mL||Max Conc. mM|
Preparing Stock Solutions
The following data is based on the product molecular weight 532.57. Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.
|Concentration / Solvent Volume / Mass||1 mg||5 mg||10 mg|
|1 mM||1.88 mL||9.39 mL||18.78 mL|
|5 mM||0.38 mL||1.88 mL||3.76 mL|
|10 mM||0.19 mL||0.94 mL||1.88 mL|
|50 mM||0.04 mL||0.19 mL||0.38 mL|
References are publications that support the biological activity of the product.
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
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
If you know of a relevant reference for GSK 1838705, please let us know.
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Keywords: GSK 1838705, GSK 1838705 supplier, GSK1838705, potent, and, selective, IR, IGF1R, inhibitors, inhibits, antitumor, insulin, receptor, like, growth, factor, 1, anaplastic, lymphoma, kinase, ALK, Insulin, Insulin-like, Receptors, insulin-like, 5111, Tocris Bioscience
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Literature in this Area
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Peptides Involved in Appetite Modulation Scientific Review
Written by Sonia Tucci, Lynsay Kobelis and Tim Kirkham, this review provides a synopsis of the increasing number of peptides that have been implicated in appetite regulation and energy homeostasis; putative roles of the major peptides are outlined and compounds available from Tocris are listed.