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LY 2109761 New
Biological Activity for LY 2109761
LY 2109761 is a selective dual TGF-β receptor type I and II (TβRI/II) inhibitor (Ki values are 38 and 300 nM in a cell-free assay, respectively); it inhibits the kinase activity of both TGF-βRI and TGF-βRII. In vitro, it significantly inhibits the growth, motility, and invasiveness of L3.6pl/GLT pancreatic cancer cells and completely suppresses TGF-β-induced Smad2 phosphorylation. In vivo, LY 2109761, in combination with Gemcitabine, significantly reduces tumor volume and spontaneous abdominal metastases in a murine model of metastatic pancreatic cancer. LY 2109761 is orally bioavailable.
Technical Data for LY 2109761
|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 LY 2109761
|Solvent||Max Conc. mg/mL||Max Conc. mM|
|DMSO||8.83||20 with gentle warming|
|ethanol||8.83||20 with gentle warming|
Preparing Stock Solutions for LY 2109761
The following data is based on the product molecular weight 441.53. 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|
|0.2 mM||11.32 mL||56.62 mL||113.24 mL|
|1 mM||2.26 mL||11.32 mL||22.65 mL|
|2 mM||1.13 mL||5.66 mL||11.32 mL|
|10 mM||0.23 mL||1.13 mL||2.26 mL|
References for LY 2109761
References are publications that support the biological activity of the product.
Melisi et al (2008) LY2109761, a novel transforming growth factor beta receptor type I and type II dual inhibitor, as a therapeutic approach to suppressing pancreatic cancer metastasis. Mol.Cancer Ther. 7 829 PMID: 18413796
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Citations for LY 2109761
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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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Stem Cells Scientific Review
Written by Kirsty E. Clarke, Victoria B. Christie, Andy Whiting and Stefan A. Przyborski, this review provides an overview of the use of small molecules in the control of stem cell growth and differentiation. Key signaling pathways are highlighted, and the regulation of ES cell self-renewal and somatic cell reprogramming is discussed. Compounds available from Tocris are listed.