PF-06447475

SKU: orb1306636

Description

PF-06447475

Research Area

Cell Biology

Key Properties

• CAS Number: 1527473-33-1
• MW: 305.33
• Purity: 99.62%
• Formula: C₁₇H₁₅N₅O
• SMILES: N#Cc1cccc(c1)-c1c[nH]c2ncnc(N3CCOCC3)c12
• Target: LRRK2
• Solubility: DMSO:15.3 mg/mL (50.11 mM);10% DMSO+40% PEG300+5% Tween 80+45% Saline:2.5 mg/mL (8.19 mM)

Bioactivity

• Target IC50:
  LRRK2 (G2019S):11nM|LRRK2:3nM
• In Vivo:
  In G2019S BAC-transgenic mice, PF-06447475 (100 mg/kg, p.o.) inhibits pS935 and pS1292 phosphorylation of LRRK2 with IC50 of 103 nM and 21 nM, respectively. In G2019S-LRRK2 rats, PF-06447475 (30 mg/kg, p.o.) blocks α-synuclein-induced dopaminergic neurodegeneration and attenuates neuroinflammation associated with G2019S-LRRK2 expression.
• In Vitro:
  In the macrophage cell line Raw264.7, PF-06447475 inhibits endogenous LRRK2 kinase activity with IC50 of <10 nM. In astrocytes, PF-06447475 rescues LRRK2 mutation-induced defects in lysosomal morphology and function.

Storage & Handling

• Storage: Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

Leucine-rich repeat kinase 2, G2019S LRRK2, LRRK2, Inhibitor, inhibit, PF06447475, PF-06447475, PF 06447475

Compound Identifiers

PubChem CID

72706840