Name: PF-06447475
Brand: Selleck Chemicals
SKU: S8202
Rating: 5 (1 reviews)

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Quality Control

Batch: Purity: 99.97%

99.97

Related Targets	CXCR Autophagy Nrf2 Mitophagy ULK FKBP Heme Oxygenase cGAS LC3 Cell wall
Other LRRK2 Inhibitors	LRRK2-IN-1 GNE-0877 (DNL201) GNE-7915 GSK2578215A MLi-2 PFE-360 GNE-9605 CZC-54252 CZC-25146 HG-10-102-01

Chemical Information, Storage & Stability

Molecular Weight	305.33	Formula	C₁₇H₁₅N₅O	Storage (From the date of receipt)	3 years-20°Cpowder
CAS No.	1527473-33-1	Download SDF		Storage of Stock Solutions	1 year-80°Cin solvent 1 month-20°Cin solvent
Synonyms	N/A			Smiles	C1COCCN1C2=NC=NC3=C2C(=CN3)C4=CC=CC(=C4)C#N

Solubility

In vitro
Batch:

DMSO : 61 mg/mL (199.78 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Water : Insoluble

Ethanol : Insoluble

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
=	×	×

Dilution Calculator Molecular Weight Calculator

In vivo Batch:
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	3.050mg/ml (9.99mM)	Taking the 1 mL working solution as an example, add 50 μL of 61 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.
Clear solution	5% DMSO 1 95% Corn oil Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	0.430mg/ml (1.41mM)	Taking the 1 mL working solution as an example, add 50 μL of 8.6 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results.

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

Dosage: mg/kg Average weight of animals: g Dosing volume per animal:μL Number of animals:

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO + % + % Tween 80 + % ddH₂O

%DMSO+ %

Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH₂O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.

Mechanism of Action

Targets/IC₅₀/Ki	LRRK2 (Cell-free assay) 3nM G2019S LRRK2 (Cell-free assay) 11nM
In vitro	In the macrophage cell line Raw264.7, PF-06447475 inhibits endogenous LRRK2 kinase activity with IC50 of <10 nM. In astrocytes, this compound rescues LRRK2 mutation-induced defects in lysosomal morphology and function.
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, this compound (30 mg/kg, p.o.) blocks α-synuclein-induced dopaminergic neurodegeneration and attenuates neuroinflammation associated with G2019S-LRRK2 expression.
References	[1] https://pubmed.ncbi.nlm.nih.gov/25353650/ [2] https://pubmed.ncbi.nlm.nih.gov/26078453/ [3] https://pubmed.ncbi.nlm.nih.gov/26251043/

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PF-06447475 LRRK2 inhibitor

Chemical Structure

Molecular Weight: 305.33