LY 2109761

Product Description

LY 2109761 is a selective dual TGF-β receptor type I and II (TβRI/II) inhibitor (K_i 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.

Solubility

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 all affect the solvent volumes required to prepare stock solutions.

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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

Calculators

Background References

References are publications that support the biological activity of the product.

• Melisi 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. 2008 PMID: 18413796