LY 2109761

Pricing Availability   Qty
Description: Selective TGF-β kinase inhibitor
Chemical Name: 4-[5,6-Dihydro-2-(2-pyridinyl)-4H-pyrrolo[1,2-b]pyrazol-3-yl]-7-[2-(4-morpholinyl)ethoxy]quinoline
Purity: ≥98% (HPLC)
Datasheet
Citations
Reviews
Literature (3)
Pathways (1)

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

M. Wt 441.53
Formula C26H27N5O2
Storage Store at -20°C
Purity ≥98% (HPLC)
CAS Number 700874-71-1
PubChem ID 11655119
InChI Key IHLVSLOZUHKNMQ-UHFFFAOYSA-N
Smiles N1=CC=CC=C1C2=NN3C(=C2C=4C=CN=C5C=C(OCCN6CCOCC6)C=CC54)CCC3

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
Solubility
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.

Select a batch to recalculate based on the batch molecular weight:
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

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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


If you know of a relevant reference for LY 2109761, please let us know.

View Related Products by Product Action

View all TGF-β Receptor Inhibitors

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Citations for LY 2109761

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Literature in this Area

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Stem Cell Research Product Guide

Stem Cell Research Product Guide

This product guide provides a background to the use of small molecules in stem cell research and lists over 200 products for use in:

  • Self-renewal and Maintenance
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Stem Cells Scientific Review

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.

Stem Cells Poster

Stem Cells Poster

Written by Rebecca Quelch and Stefan Przyborski from Durham University (UK), this poster describes the isolation of pluripotent stem cells, their maintenance in culture, differentiation, and the generation and potential uses of organoids.

Pathways for LY 2109761

TGF-β Signaling Pathway

TGF-β Signaling Pathway

The TGF-β signaling pathway is involved in the regulation of growth and proliferation of cells along with migration, differentiation and apoptosis.