Biological Activity
Potent and selective PAK1 inhibitor (IC50 = 5 nM). Selective for PAK1 over PAK2 and a panel of 442 kinases. Inhibits autophosphorylation of PAK1 in KRAS-mutated pancreatic cancer cell lines.
Licensing Information
This probe is supplied in conjunction with the Structural Genomics Consortium. For further characterization details, please visit the NVS-PAK1-1 probe summary on the SGC website.
Technical Data
| M. Wt | 479.93 |
| Formula | C23H25ClF3N5O |
| Storage | Store at -20°C |
| Purity | ≥98% (HPLC) |
| CAS Number | 1783816-74-9 |
| Smiles | FC(F)CN(C(C=CC(F)=C1)=C1N=C2N[C@H]3CCN(C(NC(C)C)=O)C3)C4=C2C=C(Cl)C=C4 |
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 | |||
| 1eq. HCl | 47.99 | 100 | |
| DMSO | 47.99 | 100 | |
| ethanol | 47.99 | 100 |
Preparing Stock Solutions
The following data is based on the product molecular weight 479.93. 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 | 2.08 mL | 10.42 mL | 20.84 mL |
| 5 mM | 0.42 mL | 2.08 mL | 4.17 mL |
| 10 mM | 0.21 mL | 1.04 mL | 2.08 mL |
| 50 mM | 0.04 mL | 0.21 mL | 0.42 mL |
Molarity Calculator
Reconstitution Calculator
Dilution Calculator
Product Datasheets
References
References are publications that support the products' biological activity.
Karpov et al (2015) Optimization of a dibenzodiazepine hit to a potent and selective allosteric PAK1 inhibitor. ACS Med.Chem.Lett. 6 776 PMID: 26191365
Keywords: NVS PAK1 1, supplier, NVSPAK11, P21-activated, kinases, PAK1, inhibitors, inhibits, potent, selective, P21-activated, Kinases, P21-activated, Kinases, Tocris Bioscience
