Biological Activity
Potent inhibitor of focal adhesion kinase (FAK); prevents FAK autophosphorylation at the Y397 site (IC50 ~ 50 nM in an in vitro kinase assay). Displays selectivity for FAK over a panel of other kinases (concentration used in assay = 1 μM). Decreases cell viability in a number of cancer cell lines; blocks colony formation in SW620 and BT474 cell lines.
Compound Libraries
Y 11 is also offered as part of the Tocriscreen Plus and Tocriscreen Kinase Inhibitor Toolbox II. Find out more about compound libraries available from Tocris.
Technical Data
| M. Wt | 265.15 |
| Formula | C8H17N4OBr |
| Storage | Store at -20°C |
| CAS Number | 1086639-59-9 |
| PubChem ID | 24195918 |
| InChI Key | HBPXFHNNLMCUPA-UHFFFAOYSA-M |
| Smiles | OCC[N+]1(CN3C2)CN(C3)CN2C1.[Br-] |
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
All Tocris products are intended for laboratory research use only.
Solubility Data
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 26.52 | 100 | |
| water | 26.52 | 100 |
Preparing Stock Solutions
The following data is based on the product molecular weight 265.15. Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 3.77 mL | 18.86 mL | 37.71 mL |
| 5 mM | 0.75 mL | 3.77 mL | 7.54 mL |
| 10 mM | 0.38 mL | 1.89 mL | 3.77 mL |
| 50 mM | 0.08 mL | 0.38 mL | 0.75 mL |
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Product Datasheets
References
References are publications that support the products' biological activity.
Golubovskaya et al (2012) A small molecule focal adhesion kinase (FAK) inhibitor, targeting Y397 site: 1-(2-hydroxyethyl) -3, 5, 7-triaza-1-azoniatricyclo [3.3.1.13,7]decane; bromide effectively inhibits FAK autophosphorylation activity and decreases cancer cell viability, clonoge Carcinogenesis PMID: 22402131
Golubovskaya et al (2008) A small molecule inhibitor, 1,2,4,5-benzenetetraamine tetrahydrochloride, targeting the Y397 site of focal adhesion kinase decreases tumor growth. J.Med.Chem. 51 7405 PMID: 18989950
Keywords: Y 11, supplier, potent, focal, adhesion, kinase, FAK, inhibits, inhibitors, autophosphorylation, selective, Y11, Focal, Adhesion, Kinase, Focal, Adhesion, Kinase, Tocris Bioscience
