PF 06447475

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Cat.No. 5716 - PF 06447475 | C17H15N5O | CAS No. 1527473-33-1
Description: Potent LRRK2 inhibitor; neuroprotective
Chemical Name: 3-[4-(4-Morpholinyl)-7H-pyrrolo[2,3-d]pyrimidin-5-yl]benzonitrile
Purity: ≥98% (HPLC)
Datasheet
Citations
Reviews
Literature

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
0.5 mM 6.55 mL 32.75 mL 65.5 mL
2.5 mM 1.31 mL 6.55 mL 13.1 mL
5 mM 0.66 mL 3.28 mL 6.55 mL
25 mM 0.13 mL 0.66 mL 1.31 mL

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References

References are publications that support the biological activity of the product.

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


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