LY 2109761

Name: LY 2109761
Brand: Tocris Bioscience
SKU: 7864

Tocris Bioscience, part of Bio-Techne | Catalog # 7864

Citations (3)

COA / SDS

Selective TGF-β kinase inhibitor

Key Product Details

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)
Molecular Weight:	441.53

View Full Technical Details for LY 2109761

Technical Data
Citations

Biological Activity for LY 2109761

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.

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 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.

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 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