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Biological Activity for Linsitinib
Linsitinib is a potent and selective dual inhibitor of the IGF-1 receptor (IC50 = 35 nM) and insulin receptor (IC50 = 75 nM); it inhibits ligand-dependent auto-phosphorylation of both receptor tyrosine kinases and prevents ligand-induced activation of downstream pathways including pAKT, pERK1/2 and p-p70S6K. The compound is selective for IGF-1R, IR and IRR in a panel of 88 kinases. Lisintinib inhibits proliferation in a variety of tumor cell lines and shows robust in vivo antitumor efficacy in an IGF-1R-driven LSN xenograft model. Orally bioavailable.
Technical Data for Linsitinib
|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 Linsitinib
|Solvent||Max Conc. mg/mL||Max Conc. mM|
Preparing Stock Solutions for Linsitinib
The following data is based on the product molecular weight 421.49. 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||2.37 mL||11.86 mL||23.73 mL|
|5 mM||0.47 mL||2.37 mL||4.75 mL|
|10 mM||0.24 mL||1.19 mL||2.37 mL|
|50 mM||0.05 mL||0.24 mL||0.47 mL|
References for Linsitinib
References are publications that support the biological activity of the product.
Mulvihill et al (2009) Discovery of OSI-906: a selective and orally efficacious dual inhibitor of the IGF-1 receptor and insulin receptor. Future Med.Chem. 1 1153 PMID: 21425998
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Citations for Linsitinib
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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!
*Please note that Tocris will only send literature to established scientific business / institute addresses.
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.