GW 788388

Key Product Details

Product Description

GW 788388 is a potent inhibitor of transforming growth factor-β type I receptor (ALK5) (IC₅₀ values are 18 and 93 nM for ALK5 binding and for TGF-β cellular assay respectively). Inhibits esophageal squamous cell carcinoma (ESCC)-induced neoangiogenesis. Reduces renal fibrosis in vivo. Orally active.

Licensing Information

Sold for research purposes under agreement from GlaxoSmithKline

Product Specifications for GW 788388

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.

Solubility

Preparing Stock Solutions for GW 788388

The following data is based on the product molecular weight 425.48.

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	2.35 mL	11.75 mL	23.50 mL
5 mM	0.47 mL	2.35 mL	4.70 mL
10 mM	0.24 mL	1.18 mL	2.35 mL
50 mM	0.05 mL	0.24 mL	0.47 mL

Calculators

Background References

References are publications that support the biological activity of the product. See our Citations tab to view 19 publications citing the usage of this product.

• Petersen Oral administration of GW788388, an inhibitor of TGF-beta type I and II receptor kinases, decreases renal fibrosis. Kidney Int. 2008 PMID: 18075500
• Noma The essential role of fibroblasts in esophageal squamous carcinoma-induced angiogenesis. Gastroenterology 2008 PMID: 18439605
• Gellibert Discovery of 4-{4-[3-(pyridin-2-yl)-1H-pyrazol-4-yl]pyridin-2-yl}-N-(tetrahydro-2H- pyran-4-yl)benzamide (GW788388): a potent, selective, and orally active transforming growth factor-β type I receptor inhibitor. J.Med.Chem. 2006 PMID: 16570917
• Tan Targeted inhibition of AVNreceptor-like kinase 5 signaling attenuates cardiac dysfunction following myocardial infarction. Am.J.Physiol.Heart Circ.Physiol. 2010 PMID: 20154262

Product Documents for GW 788388