Biological Activity
Potent group I PAK inhibitor (IC50 values are 8, 13 and 19 nM for PAK1, 2 and 3, respectively). Exhibits significant inhibition of YES1, RET, CSF1R and TEK at 100 nM, but is inactive against group II PAK isoforms (IC50 >10 μM for PAK4). Inhibits proliferation of pancreatic cancer and schwannoma cells in vitro and exhibits antitumor effects in mice.
Technical Data
| M. Wt | 558.1 |
| Formula | C29H28ClN7OS |
| Storage | Store at -20°C |
| Purity | ≥98% (HPLC) |
| CAS Number | 1286739-19-2 |
| PubChem ID | 70934541 |
| InChI Key | DHUJCQOUWQMVCG-UHFFFAOYSA-N |
| Smiles | CN(CC1)CCN1C2=CC=C(NC3=NC(N(CC)C(C(C4=CC=C(C5=CN=CS5)C=C4Cl)=C6)=O)=C6C=N3)C=C2 |
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 | 11.16 | 20 |
Preparing Stock Solutions
The following data is based on the product molecular weight 558.1. 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 | 1.79 mL | 8.96 mL | 17.92 mL |
| 5 mM | 0.36 mL | 1.79 mL | 3.58 mL |
| 10 mM | 0.18 mL | 0.9 mL | 1.79 mL |
| 50 mM | 0.04 mL | 0.18 mL | 0.36 mL |
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Product Datasheets
References
References are publications that support the products' biological activity.
Licciulli et al (2013) FRAX597, a small molecule inhibitor of the p21-activated kinases, inhibits tumorigenesis of neurofibromatosis type 2 (NF2)-associated Schwannomas. J.Biol.Chem. 288 29105 PMID: 23960073
Yeo et al (2016) FRAX597, a PAK1 inhibitor, synergistically reduces pancreatic cancer growth when combined with gemcitabine. BMC Cancer 16 24 PMID: 26774265
Keywords: FRAX 597, supplier, FRAX597, potent, group, I, PAK, inhibits, inhibitors, p21, activated, kinase, P21-activated, Kinases, P21-activated, Kinases, Tocris Bioscience
