Biological Activity
Selective focal adhesion kinase (FAK) inhibitor that displays no significant activity at a range of other kinases including EGFR, PDGFR and IGF-RI. Prevents FAK autophosphorylation at Y397 (IC50 = 1 μM), promotes cell detachment and inhibits cell adhesion in vitro. Exhibits antiproliferative activity in a variety of human tumor cell lines in vitro and in breast cancer cells in vivo.
Technical Data
| M. Wt | 284.01 |
| Formula | C6H10N4.4HCl |
| Storage | Desiccate at RT |
| CAS Number | 4506-66-5 |
| PubChem ID | 78260 |
| InChI Key | BZDGCIJWPWHAOF-UHFFFAOYSA-N |
| Smiles | NC1=C(N)C=C(N)C(N)=C1.Cl.Cl.Cl.Cl |
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 | 21.3 | 75 | |
| ethanol | 1.42 | 5 | |
| water | 14.2 | 50 |
Preparing Stock Solutions
The following data is based on the product molecular weight 284.01. 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 | 3.52 mL | 17.61 mL | 35.21 mL |
| 5 mM | 0.7 mL | 3.52 mL | 7.04 mL |
| 10 mM | 0.35 mL | 1.76 mL | 3.52 mL |
| 50 mM | 0.07 mL | 0.35 mL | 0.7 mL |
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References
References are publications that support the products' biological activity.
Golubovskaya et al (2008) A small molecule inhibitor, 1,2,4,5-benzenetetraamine tetrahydrochloride, targeting the Y397 site of focal adhesion kinase decreases tumour growth. J.Med.Chem. 51 7405 PMID: 18989950
Hochwald et al (2009) A novel small molecule inhibitor of FAK decreases growth of human pancreatic cancer. Cell Cycle 8 2435 PMID: 19571674
Keywords: FAK Inhibitor 14, supplier, Selective, FAK, inhibitors, inhibits, Focal, Adhesion, Kinases, Inhibitor14, Y15, NSC, 677249, Focal, Adhesion, Kinase, Focal, Adhesion, Kinase, Tocris Bioscience
