LY 364947

Product Description

LY 364947 is a selective inhibitor of TGF-β type-I receptor (TGF-β RI, TGFR-I, TβR-I, ALK-5) (IC₅₀ values are 59, 400 and 1400 nM for TGR-β RI, TGF-β RII and MLK-7K respectively). Inhibits TGF-β-dependent luciferase production in mink lung cells (p3TP lux) and growth in mouse fibroblasts (NIH 3T3) (IC₅₀ values are 47 and 89 nM respectively). Suppresses invasion of MDA-MB-231 breast cancer cells in a matrigel invasion assay.

Solubility

Preparing Stock Solutions for LY 364947

The following data is based on the product molecular weight 272.31

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.

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

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Concentration / Solvent Volume / Mass	1 mg	5 mg	10 mg
1 mM	3.67 mL	18.36 mL	36.72 mL
5 mM	0.73 mL	3.67 mL	7.34 mL
10 mM	0.37 mL	1.84 mL	3.67 mL
50 mM	0.07 mL	0.37 mL	0.73 mL

Calculators

Background References

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

• Li Dihydropyrrolopyrazole transforming growth factor-β type I receptor kinase domain inhibitors: a novel benzimidazole series with selectivity versus transforming growth factor-β type II receptor kinase and mixed lineage kinase 7. J.Med.Chem. 2006 PMID: 16539403
• Shiou Smad4-dependent regulation of urok. plasminogen activator secretion and RNA stability associated with invasiveness by autocrine and paracrine transforming growth factor-β. J.Biol.Chem. 2006 PMID: 16959768
• Sawyer Synthesis and activity of new aryl- and heteroaryl-substituted pyrazole inhibitors of the transforming growth factor-μ type I receptor kinase domain. J.Med.Chem. 2003 PMID: 12954047