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GW 788388

Cat. No. 3264

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Chemical Name: 4-[4-[3-(2-Pyridinyl)-1H-pyrazol-4-yl]-2-pyridinyl]-N-(tetrahydro-2H-pyran-4-yl)-benzamide

Biological Activity

Selective inhibitor of transforming growth factor-β type I receptor (ALK5) (IC₅₀ values are 0.018 and 0.093 μM for ALK5 binding and for TGF-β cellular assay respectively). Inhibits esophageal squamous cell carcinoma (ESCC)-induced neoangiogenesis. Orally active.

Licensing Information

Sold for research purposes under agreement from GlaxoSmithKline

Technical Data

M.Wt:

425.48

Formula:

C₂₅H₂₃N₅O₂

Solubility:

Soluble to 100 mM in DMSO

Purity:

>98 %

Storage:

Store at +4°C

CAS No:

452342-67-5

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

Resources

Certificate of Analysis / Safety Data Sheet

Certificate of Analysis: View current batch

Safety Data Sheet: View Safety Data Sheet

References

Gellibert et al (2006) 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. 49 2210. PMID: 16570917.

Noma et al (2008) The essential role of fibroblasts in esophageal squamous carcinoma-induced angiogenesis. Gastroenterology 134 1981. PMID: 18439605.

Tan et al (2010) Targeted inhibition of activin receptor-like kinase 5 signaling attenuates cardiac dysfunction following myocardial infarction. Am.J.Physiol.Heart Circ.Physiol. 298 H1415. PMID: 20154262.

If you know of a relevant citation for this product please let us know.

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Keywords: GW 788388, supplier, GW788388, transforming, growth, factor, type, I, receptors, tgfbeta, tgfb, tgfβ, inhibitors, TGF-βRI

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