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Biological Activity for GSK 1838705
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.
Sold for research purposes under agreement from GlaxoSmithKline.
Compound Libraries for GSK 1838705
Technical Data for GSK 1838705
|Storage||Store at -20°C|
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.
Solubility Data for GSK 1838705
|Solvent||Max Conc. mg/mL||Max Conc. mM|
Preparing Stock Solutions for GSK 1838705
The following data is based on the product molecular weight 532.57. Batch specific molecular weights may vary from batch to batch due to the degree 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 for GSK 1838705
References are publications that support the biological activity of the product.
Sabbatini et al (2009) GSK1838705A inhibits the Ins-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
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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
1 Citation for GSK 1838705
Citations are publications that use Tocris products. Selected citations for GSK 1838705 include:
William B et al (2017) Insulin fine-tunes self-renewal pathways governing naive pluripotency and extra-embryonic endoderm. Nat Cell Biol 19 1164-1177 PMID: 28945231
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Literature in this Area
Tocris offers the following scientific literature in this area to showcase our products. We invite you to request* your copy today!
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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.