PF-06447475

• CAT Number: I001901
• CAS Number: 1527473-33-1
• Molecular Formula: C₁₇H₁₅N₅O
• Molecular Weight: 305.33
• Purity: ≥95%
• Target: LRRK2
• Solubility: DMSO: ≥ 33 mg/mL
• Storage: room temp
• IC50: 3 nM/11 nM(Wt LRRK2/G2019S LRRK2)
• IUPAC Name: 3-(4-morpholin-4-yl-7H-pyrrolo[2,3-d]pyrimidin-5-yl)benzonitrile
• InChI: InChI=1S/C17H15N5O/c18-9-12-2-1-3-13(8-12)14-10-19-16-15(14)17(21-11-20-16)22-4-6-23-7-5-22/h1-3,8,10-11H,4-7H2,(H,19,20,21)
• InChIKey: BHTWDJBVZQBRKP-UHFFFAOYSA-N
• SMILES: C1COCCN1C2=NC=NC3=C2C(=CN3)C4=CC=CC(=C4)C#N

PF-06447475（Cat No.:I001901） is a highly potent, selective, and brain-penetrating inhibitor of the leucine-rich repeat kinase 2 (LRRK2) kinase. It exhibits impressive inhibitory activity with an IC50 (half-maximal inhibitory concentration) of 3 nM. The selective targeting of LRRK2, a protein kinase associated with neurodegenerative disorders like Parkinson’s disease, makes PF-06447475 a promising therapeutic candidate for the treatment of such conditions.

Reference

1:Neuroprotective Effect of the LRRK2 Kinase Inhibitor PF-06447475 in Human Nerve-Like Differentiated Cells Exposed to Oxidative Stress Stimuli: Implications for Parkinson/’s Disease. Mendivil-Perez M, Velez-Pardo C, Jimenez-Del-Rio M.Neurochem Res. 2016 Oct;41(10):2675-2692. Epub 2016 Jul 9. PMID: 27394417 2: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. Henderson JL, Kormos BL, Hayward MM, Coffman KJ, Jasti J, Kurumbail RG, Wager TT, Verhoest PR, Noell GS, Chen Y, Needle E, Berger Z, Steyn SJ, Houle C, Hirst WD, Galatsis P.J Med Chem. 2015 Jan 8;58(1):419-32. doi: 10.1021/jm5014055. Epub 2014 Nov 17. PMID: 25353650