GW 788388
Tocris Bioscience, part of Bio-Techne | Catalog # 3264
Potent and selective inhibitor of TGF-βRI
Key Product Details
Description
Potent and selective inhibitor of TGF-βRI
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 GlaxoSmithKlineProduct Specifications
Molecular Weight
425.48
Formula
C25H23N5O2
Storage
Store at +4°C
Purity
≥98% (HPLC)
Chemical Name
4-[4-[3-(2-Pyridinyl)-1H-pyrazol-4-yl]-2-pyridinyl]-N-(tetrahydro-2H-pyran-4-yl)-benzamide
CAS Number
452342-67-5
PubChem ID
10202642
InChI Key
SAGZIBJAQGBRQA-UHFFFAOYSA-N
SMILES
O=C(NC5CCOCC5)C(C=C4)=CC=C4C1=CC(C2=CNN=C2C3=CC=CC=N3)=CC=N1
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Solubility
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 42.55 | 100 |
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.
| 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
Molarity Calculator
Dilution Calculator
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Background References
References are publications that support the biological activity of the 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 Specific Notices for GW 788388
For research use only
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