Biological Activity
Potent LRRK2 inhibitor (IC50 = 3 nM). Attenuates α-synuclein-induced dopaminergic neurodegeneration and neuroinflammation in G2019S-LRRK2 expressing rats. Also neuroprotective in wild type rats. Brain penetrant.
Licensing Information
Sold for research purposes under agreement from Pfizer Inc
Compound Libraries
PF 06447475 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 | 305.33 |
| Formula | C17H15N5O |
| Storage | Store at +4°C |
| Purity | ≥98% (HPLC) |
| CAS Number | 1527473-33-1 |
| PubChem ID | 72706840 |
| InChI Key | BHTWDJBVZQBRKP-UHFFFAOYSA-N |
| Smiles | N#CC1=CC(C3=CNC2=NC=NC(N4CCOCC4)=C23)=CC=C1 |
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 | 15.27 | 50 |
Preparing Stock Solutions
The following data is based on the product molecular weight 305.33. 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 | 3.28 mL | 16.38 mL | 32.75 mL |
| 5 mM | 0.66 mL | 3.28 mL | 6.55 mL |
| 10 mM | 0.33 mL | 1.64 mL | 3.28 mL |
| 50 mM | 0.07 mL | 0.33 mL | 0.66 mL |
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Product Datasheets
References
References are publications that support the products' biological activity.
Daher et al (2015) Leucine-rich repeat kinase 2 (LRRK2) pharmacological inhibition abates α-synuclein gene-induced neurodegeneration. J.Biol.Chem. 290 19433 PMID: 26078453
Henderson et al (2015) Discovery and preclinical profiling of 3-[4-(morpholin-4-yl)-7H-pyrrolo[2,3-d]pyrimidin-5-yl]benzonitrile (PF-06447475), a highly potent, selective, brain penetrant, and in vivo active LRRK2 kinase inhibitor. J.Med.Chem. 58 419 PMID: 25353650
Keywords: PF 06447475, supplier, PF06447475, potent, LRRK2, inhibitors, inhibits, neurodegeneration, neuroinflammation, brain, penetrant, LRRK2, LRRK2, Tocris Bioscience
